Epigenetics
Epigenetics research delves into the molecular mechanisms that control gene expression and cellular traits without altering the underlying DNA sequence. One crucial aspect of this field is the role of small molecules, which act as powerful regulators of epigenetic modifications. These small compounds, typically comprising a few dozen to a few hundred atoms, have emerged as essential tools in understanding and manipulating the epigenome.
- DNA Methylation Inhibitors: Small molecules like 5-azacytidine and 5-aza-2'-deoxycytidine are DNA methyltransferase inhibitors. They block the addition of methyl groups to DNA, leading to DNA demethylation. This can reactivate silenced genes, potentially offering therapeutic avenues for conditions like cancer.
- HDAC inhibitors: HDACs remove acetyl groups from histone proteins, contributing to gene repression. Small molecule HDAC inhibitors, such as Vorinostat and Romidepsin, can reverse this process by increasing histone acetylation, allowing genes to be more accessible for transcription. These inhibitors are being explored for cancer therapy and other conditions.
- Histone Methyltransferase Inhibitors: Small molecules like GSK126 inhibit specific histone methyltransferases, affecting histone methylation patterns. This can alter gene expression, making them promising candidates for cancer and other diseases with epigenetic dysregulation.
- RNA Modulators: Small molecules can also target non-coding RNAs involved in epigenetic regulation. For instance, small molecules called small interfering RNAs (siRNAs) can be designed to target and degrade specific long non-coding RNAs, influencing gene expression.
- Epigenetic Reader Domain Inhibitors: These small molecules target proteins that recognize and bind to specific epigenetic marks. Examples include inhibitors of bromodomain-containing proteins (BET inhibitors), which can disrupt gene regulation by interfering with protein-DNA interactions.
Small molecules in epigenetics research not only provide insights into the fundamental biology of gene regulation but also hold immense promise for developing novel therapeutics. Their ability to selectively modulate specific epigenetic marks and pathways has led to ongoing clinical trials and drug development efforts for various diseases, including cancer, neurological disorders, and inflammatory conditions. Understanding and harnessing the power of these small molecules is at the forefront of modern epigenetics research, offering new hope for precision medicine and targeted therapies.
3 key components involved in the regulation of epigenetic modifications
Epigenetics Writer
Epigenetics writers are enzymes responsible for adding chemical marks or modifications to DNA or histone proteins. These marks include DNA methylation (addition of methyl groups to DNA) and histone modifications (such as acetylation, methylation, phosphorylation, etc.).
Epigenetics Reader
Function: Epigenetics readers are proteins that can recognize and bind to specific epigenetic marks on DNA or histones. These reader proteins interpret the epigenetic code and facilitate downstream cellular processes, such as gene activation or repression.
Epigenetics Eraser
Function: Epigenetics erasers are enzymes responsible for removing or reversing epigenetic marks on DNA or histones. This process allows for the dynamic regulation of gene expression and the resetting of epigenetic states during various stages of development and in response to environmental changes.
Catalog No.
Product Name
Application
Product Information
Citations
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SMARCA2/4 Inhibitor
SMARCA2-IN-6 is a potent inhibitor of SMARCA2 and SMARCA4, exhibiting IC50 values under 5 nM for both targets. This compound effectively suppresses KRT80 gene expression in H1299 cells with an IC50 of 26 nM, and demonstrates significant antiproliferative effects in BRG1-mutant SKMEL5 cells, with an IC50 of 13 nM. SMARCA2-IN-6 serves as a valuable tool for research applications focused on chromatin remodeling and associated oncogenic pathways. -
BRD4 Inhibitor
BRD4-IN-7 is a selective inhibitor of the bromodomain-containing protein 4 (BRD4). By targeting BRD4, this compound plays a crucial role in modulating gene expression and has been shown to disrupt the interaction between BRD4 and acetylated histones. Its primary applications include cancer research and investigations into various diseases involving epigenetic regulation, making it a valuable tool for further studies on transcriptional control and associated pathways. -
BRD4-1 Inhibitor
Bromodomain inhibitor-9 is a selective inhibitor of BRD4-1, exhibiting a Kd of 12 nM. This compound has been shown to play a significant role in modulating biological pathways related to systemic and tissue inflammation, lipid metabolism, fibrosis, and chronic autoimmune diseases. Its application in research provides valuable insights into the therapeutic potential for addressing these conditions. -
BET Inhibitor
Y08060 is a selective inhibitor of Bromodomain and Extra-Terminal (BET) proteins. It demonstrates significant anti-proliferative effects on C4-2B and LNCaP prostate cancer cell lines, with IC50 values of 3.23 μM and 4.41 μM, respectively. Additionally, Y08060 effectively suppresses colony formation and androgen receptor (AR) expression in these cell lines, making it a valuable tool for research applications targeting prostate cancer biology. -
Bromodomain Inhibitor
Bromodomain inhibitor-13 is a selective inhibitor targeting bromodomain-containing proteins (BCPs), including SMARCA2, SMARCA4, and the bromodomain of PB1. It exhibits potent binding affinity with KD values of 37 nM for SMARCA2, 53 nM for SMARCA4, and 30 nM for PB1(5), alongside a KD of 190 nM for PB1(2). This compound is valuable for research into epigenetic regulation and the role of bromodomains in various cellular processes, making it a useful tool for studying gene expression modulation and protein interactions in cancer and other diseases. -
BRD4 PROTAC
WWL0245 is a highly selective BRD4 PROTAC that effectively induces degradation of BRD4 with a sub-nanomolar DC50 of less than 1 nM, while demonstrating significantly lower potency against BRD2/3 and PLK1 (DC50 > 1 μM). This compound exhibits remarkable cytotoxicity in BET inhibitor-sensitive cancer cell lines, particularly in androgen receptor-positive prostate cancer models. WWL0245 serves as a valuable research tool for exploring the biological functions of BRD4 and holds potential as a therapeutic candidate in the context of AR-positive prostate cancer. -
PROTAC BRD9 Degrader
(S,R)-CFT8634 is a selective PROTAC-class degrader targeting BRD9, designed for oral administration. This compound facilitates the ubiquitination and subsequent degradation of BRD9, which is implicated in various diseases characterized by abnormal cell proliferation. The structure comprises a BRD9 ligand, a CRBN ligase ligand, and a PROTAC linker, enabling effective recruitment of the E3 ligase for degradation. (S,R)-CFT8634 is a valuable tool for investigating BRD9-related biological processes and therapeutic strategies. -
Bromodomain Inhibitor
Bromodomain inhibitor-12 is a selective bromodomain inhibitor that interferes with the interaction between bromodomain-containing proteins and acetylated lysines. This compound exhibits significant biological activity in modulating chromatin dynamics and has potential applications in the study of autoimmune and inflammatory diseases. Its ability to inhibit bromodomain-mediated signaling pathways makes it a valuable tool for investigating therapeutic strategies in these conditions. -
BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-34 is a selective degrader that targets the bromodomain-containing protein 4 (BRD4) through a proteolysis-targeting chimera (PROTAC) mechanism. It induces the degradation of the BRD4-BD2 domain via the VHL E3 ubiquitin ligase system. This compound has significant potential for use in cancer research, enabling investigations into the therapeutic effects of targeting BRD4 in oncogenic pathways. -
BET bromodomain Ligand
TC AC 28 is a high-affinity ligand for bromodomain and extraterminal (BET) proteins, demonstrating Kd values of 40 nM for Brd2(2) and 800 nM for Brd2(1). This compound exhibits significant biological activity in regulating gene expression through the modulation of acetylated lysine recognition. TC AC 28 is applicable in research focusing on cancer, inflammation, and other diseases associated with BET protein function. -
BET Inhibitor
BRD4 Inhibitor-19 is a small molecule inhibitor targeting the bromodomain and extraterminal (BET) family, specifically inhibiting BRD4 with an IC50 of 55 nM at the BRD4-BD1 site. This compound exhibits significant anti-proliferative effects, making it a valuable tool in the study of multiple myeloma and related hematological malignancies. Researchers can utilize BRD4 Inhibitor-19 to explore the roles of BET proteins in cancer biology and evaluate potential therapeutic strategies in targeting aberrant gene expression. -
BET Inhibitor
BET-IN-27 is a potent inhibitor of bromodomain and extraterminal (BET) proteins, demonstrating IC50 values of 3.3 nM for BRD4-BD2, 3.4 nM for BRD4-BD1, 4.1 nM for BRD2-BD1, 20.4 nM for BRD3-BD1, and 42.0 nM for BRDT-BD1. This compound exhibits significant anti-proliferative effects, making it a valuable tool for research in cancer biology and therapeutic development targeting BET protein pathways. Its selective inhibition profile allows for further exploration of BET proteins in various disease models. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4 degrader-37 is a proteolysis-targeting chimera (PROTAC) that selectively degrades SMARCA2 and SMARCA4 proteins. It exhibits a potent inhibitory concentration (IC50) of ≤0.1 μM, highlighting its efficacy in disrupting these bromodomain-containing proteins. This reagent is suitable for applications in cancer research and therapeutic development, particularly in studies involving epigenetic modulation and chromatin remodeling. -
BET/BRD4 Probe
BiBET is a bivalent chemical probe targeting the BET family of bromodomain-containing proteins, specifically BRD4. It exhibits the ability to simultaneously bind to two bromodomains through a cis-binding mechanism. This unique interaction profile makes BiBET valuable for studying the role of BET proteins in cellular processes, particularly in cancer biology and inflammatory responses. Researchers can utilize BiBET to investigate the regulatory mechanisms of gene expression mediated by BRD4 and explore potential therapeutic strategies against related diseases. -
BET Inhibitor
BETi-211 is a potent BET inhibitor with a Ki value of less than 1 nM. It selectively inhibits the growth of triple-negative breast cancer (TNBC) cell lines, exhibiting an IC50 of less than 1 μM. BETi-211 effectively induces degradation of BET proteins, leading to significant suppression of tumor growth in xenograft models of breast cancer, making it a valuable tool for cancer research and therapeutic development. -
BRD4 Inhibitor
BRD4 Inhibitor-33 is a selective inhibitor of Bromodomain-containing protein 4 (BRD4), which plays a crucial role in regulating gene expression through the recognition of acetylated lysines. This compound has demonstrated significant potential in studies related to acute and chronic kidney diseases, making it valuable for researchers investigating therapeutic approaches for renal pathologies. Its mechanism of action may facilitate insights into the molecular underpinnings of kidney dysfunction and inform future treatment strategies. -
CBP/EP300 Inhibitor
I-CBP112 hydrochloride is a selective inhibitor of CBP and EP300, acting through direct binding to their bromodomains with dissociation constants of 142 nM and 625 nM, respectively. This compound has been shown to significantly diminish the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells both in vitro and in vivo, demonstrating dose-dependent efficacy. Additionally, I-CBP112 enhances the cytotoxic effects of the BET bromodomain inhibitor JQ1 and doxorubicin, making it a valuable tool for research in cancer therapeutics and epigenetic regulation. -
BRD4 Inhibitor
BRD4 Inhibitor-32 is a potent inhibitor of the Bromodomain-containing protein 4 (BRD4), targeting the interaction between BRD4 and acetylated histones. This compound exhibits significant biological activity in the modulation of inflammatory pathways and has potential applications in the study of acute and chronic kidney diseases. It serves as a valuable tool in research aimed at understanding the role of BRD4 in renal pathophysiology and therapeutic intervention. -
BET Inhibitor
BET-IN-24 is a bromodomain and extra-terminal (BET) inhibitor that selectively targets BET proteins. This compound is known to modulate gene expression and has demonstrated significant biological activity in various research contexts, including virology, heart failure, inflammation, central nervous system (CNS) diseases, and cancer. Its ability to inhibit BET proteins makes it a valuable tool for exploring the underlying mechanisms of these conditions and assessing potential therapeutic strategies. -
CBP/p300 Inhibitor
XDM-CBP is a potent inhibitor of the CBP/p300 transcriptional co-activators. This compound effectively disrupts CBP/p300-mediated signaling pathways, making it valuable for investigating the role of these proteins in various malignancies, including malignant melanoma, breast cancer, and leukemia. XDM-CBP serves as an important tool in cancer research, aiding in the understanding of tumorigenesis and potential therapeutic strategies. -
SMARCA2/4 Ligand
SMARCA2/4-ligand-5 is a selective ligand targeting the SMARCA2 and SMARCA4 proteins, functioning as a crucial component in the PROTAC SMARCA2/4 degrader-37. This compound demonstrates potent biological activity, achieving an IC50 of ≤0.1 μM, making it suitable for applications in targeted protein degradation studies. Research utilizing SMARCA2/4-ligand-5 contributes to understanding the roles of these chromatin remodelers in various biological processes and cancer biology. -
BRDT-BD2 Inhibitor
CDD-1147 is a selective inhibitor of the BRDT-BD2 domain, exhibiting an IC50 of 94 nM. This compound is primarily utilized in research investigating non-hormonal contraceptive methods for males. Its ability to hinder BRDT interactions facilitates the exploration of reproductive targets, contributing to the advancement of male contraceptive solutions. -
CBP bromodomain Inhibitor
CBP/p300-IN-24 is a selective inhibitor of the CBP bromodomain, exhibiting an IC50 of 32 μM and demonstrating notable selectivity over the BRD4 BD-1 bromodomain. This compound interacts with the acetyl lysine binding pocket, establishing hydrogen bonds with Asn1168 and a solvent-mediated hydrogen bond with Tyr1125, alongside hydrophobic interactions with Leu1120, Ile1122, and Val1174. CBP/p300-IN-24 is useful for investigating the role of CBP in various signaling pathways and disease states, particularly in cancer research and epigenetic studies. -
JAK3 Inhibitor
JAK3-IN-13 is a selective and orally bioavailable inhibitor of JAK3, exhibiting IC50 values of 4728, 2039, 8, and 365 nM against NK1, JNK2, JNK3, and Tyk2, respectively. This compound demonstrates significant antiproliferative effects and induces cell cycle arrest in the G0/G1 phase. JAK3-IN-13 is particularly relevant for research applications focused on tumor biology and the modulation of immune responses. -
PIM-3 Inhibitor
M-110 is a selective, ATP-competitive inhibitor of PIM kinases, prominently targeting PIM-3 with an IC50 of 47 nM. This compound exhibits inhibitory activity against PIM-1 and PIM-2 with IC50 values around 2.5 μM. M-110 has demonstrated efficacy in curtailing the proliferation of prostate cancer cell lines, exhibiting IC50 values ranging from 0.6 to 0.9 μM. This makes M-110 a valuable tool for studying PIM kinase signaling pathways and their role in cancer biology. -
Pim-2 Inhibitor
HJ-PI01, a potent Pim-2 inhibitor, effectively induces apoptosis and autophagic cell death in cancer cells. This compound demonstrates significant anti-tumor activity in vivo, notably inhibiting tumor growth in MDA-MB-231 xenograft mouse models. HJ-PI01 serves as a valuable tool for cancer research, facilitating investigations into the therapeutic implications of Pim-2 inhibition. -
PIM Inhibitor
Uzansertib is a potent, orally active pan-PIM kinase inhibitor that operates through ATP-competitive mechanisms, exhibiting IC50 values of 0.24 nM, 30 nM, and 0.12 nM for PIM1, PIM2, and PIM3, respectively. This compound demonstrates significant anti-proliferative activity across a range of hematologic tumor cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Researchers can utilize Uzansertib to explore the roles of PIM kinases in tumorigenesis and potential treatment strategies. -
Pim-1/2 Kinase Inhibitor
Pim-1/2 kinase inhibitor 1 is a selective inhibitor of Pim-1 and Pim-2 kinases, targeting their phosphorylation activity. This compound effectively disrupts the phosphorylation of key substrates, including 4E-BP1 and p27Kip1, which are crucial for cell cycle regulation and protein synthesis. Pim-1/2 kinase inhibitor 1 is primarily utilized in cancer research, particularly in studies focusing on the mechanisms underlying prostate cancer progression. -
PIM Inhibitor
AZD1897 is a potent inhibitor of PIM1, PIM2, and PIM3 kinases, demonstrating IC50 values of less than 3 nM for each target. This compound exhibits significant anticancer activity, particularly in acute myeloid leukemia (AML) cells, where it shows a synergistic effect when used in combination with Capivasertib. The mechanism of action involves the inhibition of critical cellular pathways, including mTOR and MCL1, making AZD1897 a valuable tool for cancer research. -
Pim Inhibitor
K00135 is a potent and selective inhibitor of PIM kinases, primarily targeting PIM1, PIM2, and PIM3. This compound demonstrates significant inhibition of cell survival and clonogenic growth in acute leukemia cells. Additionally, K00135 effectively reduces the phosphorylation of downstream targets of the PIM signaling pathway, making it a valuable tool for cancer research focusing on PIM kinase-related mechanisms. -
Pim/DAPK3 Inhibitor
HS56 is an ATP-competitive dual inhibitor of Pim kinases and DAPK3, demonstrating Ki values of 0.26 μM for DAPK3, 0.208 μM for Pim-3, and over 100 μM for Pim-2 and Pim-1. This compound effectively inhibits LC20 phosphorylation and smooth muscle contraction, leading to a reduction in blood pressure in spontaneously hypertensive mouse models. HS56 is suitable for research investigating the mechanisms and potential treatments for hypertension. -
Pim-1 Kinase Inhibitor
Pim-1 Kinase Inhibitor 13 is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 of 4.41 μM. This compound is instrumental in the study of immunological processes and cancer biology, providing valuable insights into Pim-1's role in cell survival and proliferation. Its application in research may facilitate the development of targeted therapies for malignancies associated with aberrant Pim-1 activity. -
Pim Inhibitor
DHPCC-9 is a selective inhibitor of Pim kinase, a critical regulator of cell survival and proliferation. This compound demonstrates potent biological activity in modulating cancer cell growth and has significant implications for cancer research, particularly in the investigation of therapeutic strategies targeting the Pim signaling pathway. Researchers can utilize DHPCC-9 to explore its effects on cellular responses and potential applications in developing anti-cancer therapies. -
Pim Inhibitor
R8-T198wt is a cell-permeable peptide that functions as a Pim-1 kinase inhibitor. By targeting the carboxyl-terminal region of p27Kip1, it exhibits significant anti-tumor activity. This reagent is ideal for research applications involving cancer biology and cellular signaling pathways associated with cell cycle regulation and apoptosis. -
Pan-PIM Inhibitor
GDC-0570 is a potent and selective pan-PIM inhibitor designed for oral administration. It exhibits pronounced antitumor activity and has shown synergistic effects when combined with Sotorasib in models of acquired KRAS-resistant non-small cell lung cancer (NSCLC). This compound serves as a valuable tool for investigating the role of PIM kinases in cancer biology and therapeutic resistance. -
PIM-1 Inhibitor
PIM1-IN-7 is a potent inhibitor of the PIM-1 kinase, exhibiting an IC50 of 0.67 μM. This compound demonstrates significant cytotoxicity against HCT-116 and MCF-7 cancer cell lines, with IC50 values of 42.9 μM and 7.68 μM, respectively. Its ability to selectively inhibit PIM-1 makes it a valuable tool for investigating the role of this kinase in cancer biology and for exploring potential therapeutic strategies. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 5 is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 value of 0.61 μM. This compound demonstrates significant cytotoxicity across various cancer cell lines, including HepG2, MCF-7, PC3, and HCT-116, with IC50 values ranging from 6.95 to 20.19 μM. It serves as a valuable tool for researching the modulation of Pim-1 in cancer biology and therapeutic applications. -
PIM Inhibitor
FD1024 is a potent PIM inhibitor with IC50 values of 1.96 nM, 38.9 nM, and 4.17 nM for PIM1, PIM2, and PIM3, respectively. This compound exhibits strong antiproliferative activity against various acute myeloid leukemia (AML) cell lines, showing effective concentrations of 0.16 μM, 0.12 μM, 1.05 μM, and 1.39 μM for EOL-1, MV-4-11, KG-1, and MOLM-16 cells. Additionally, FD1024 demonstrates significant antitumor efficacy in in vivo mouse models, making it a valuable tool for research into AML therapeutic strategies. -
PIM-1 Inhibitor
PIM1-IN-6 is a potent inhibitor of Pim-1 kinase, exhibiting an IC50 of 0.60 μM. This compound demonstrates significant cytotoxic activity in HCT-116 and MCF-7 cancer cell lines, with IC50 values of 1.51 μM and 15.2 μM, respectively. PIM1-IN-6 holds promise for research applications in cancer biology, particularly in studies aimed at elucidating the role of Pim-1 in tumor proliferation and survival. -
Pim-1 Kinase Inhibitor
10-DEBC is a selective inhibitor of Pim-1 kinase, demonstrating potent inhibitory activity with an IC50 of 1.28 μM. This compound plays a critical role in regulating cell proliferation and survival, making it a valuable tool for research in cancer biology and therapeutic interventions. Its specificity for Pim-1 kinase supports its use in studies exploring signal transduction pathways and the development of targeted cancer therapies. -
PIM1 Inhibitor
PIM1-IN-4 is a selective inhibitor of PIM1 kinase, demonstrating potent activity in blocking PIM1-mediated signaling. In addition to PIM1, PIM1-IN-4 exhibits significant inhibition of several other kinases, including SGK-1, PKA, CaMK-1, GSK3β, and MSK1. This compound is valuable for investigating its role in cancer biology and therapeutic strategies targeting PIM1-related pathways. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 3 (Compound H5) is a selective inhibitor of Pim-1 kinase, exhibiting an IC50 of 35.13 nM. This compound effectively modulates the activity of Pim-1, a serine/threonine kinase involved in cell growth and survival signaling pathways. It is valuable for studying the role of Pim-1 in cancer and other diseases where its dysregulation is implicated. -
Pim Inhibitor
MNK/PIM-IN-1 is a dual inhibitor targeting MNK and PIM kinases, showcasing a favorable pharmacokinetic profile. This reagent exhibits significant antitumor activity and is applicable in studying the roles of MNK and PIM signaling pathways in cancer biology. It is an essential tool for researchers investigating the mechanisms of cell proliferation and survival in various malignancies. -
PIM1 Inhibitor
NMS-P645 is a potent PIM1 inhibitor that exhibits anti-proliferative activity, particularly when used in combination with GDC-0941 in both TMPRSS2/ERG positive and negative prostate cancer cells. By reversing PIM1-induced pro-survival signals, NMS-P645 contributes valuable insights into the mechanisms underlying prostate cancer resistance and cell survival. This compound is suitable for research applications focused on prostate cancer treatment and the exploration of PIM1 signaling pathways. -
Pim-1 Kinase Inhibitor
Pim-1 kinase inhibitor 4 is a potent inhibitor of Pim-1 kinase, with an inhibitory concentration (IC50) of 17.01 nM. This compound exhibits antioxidant activity and inhibits DPPH, contributing to its biological profile. Additionally, Pim-1 kinase inhibitor 4 induces apoptosis in PC-3 prostate cancer cells, demonstrating an IC50 of 16 nM for growth inhibition. This reagent is valuable for research focused on prostate cancer and cellular apoptosis mechanisms. -
Pim-2 Inhibitor
PIM-IN-2 is a potent inhibitor of Pim-2 kinases, exhibiting an IC50 of 25 nM. This compound has demonstrated significant antiapoptotic properties and promotes cell survival, making it a valuable tool in cancer research. Its elevated expression in various human tumors positions PIM-IN-2 as a relevant reagent for studies on tumor biology and therapeutic strategies targeting the Pim kinase pathway. -
Pim-1 Inhibitor
Pim-1 kinase inhibitor 6 is a selective inhibitor of Pim-1 kinase, demonstrating an IC50 value of 0.46 μM. This compound exhibits significant cytotoxic activity against various cancer cell lines, making it a valuable tool for cancer research. Its ability to target and inhibit Pim-1 kinase contributes to its potential applications in investigating therapeutic strategies for malignancies. -
Pim Inhibitor
PIM-IN-4 is a potent inhibitor of Pim kinases, exhibiting Ki values of 2 nM, 3 nM, and 0.5 nM for Pim-1, Pim-2, and Pim-3, respectively. By inhibiting the phosphorylation of the pro-apoptotic protein Bad, PIM-IN-4 effectively induces apoptosis in leukemic cells. This compound is valuable for research into leukemia and related signaling pathways, contributing to the understanding of therapeutic strategies in hematological malignancies. -
PIM-1/PIM-2 Inhibitor
Pim-1/2 kinase inhibitor 2 is a selective competitive inhibitor of PIM-1 and PIM-2 kinases, with IC50 values of 1.31 μM and 0.67 μM, respectively. This compound exhibits low cytotoxicity in normal human lung fibroblast Wi-38 cells while demonstrating potent anticancer activity against various cancer cell lines, including myeloid leukemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2). It serves as a valuable tool for studying the therapeutic potential of PIM inhibition in cancer research. -
Selective Hhat Inhibitor
RU-SKI 43 hydrochloride is a selective inhibitor of Hedgehog acyltransferase (Hhat) with an IC50 of 850 nM. This compound effectively reduces Gli-1 activation via Smoothened-independent, non-canonical signaling pathways and inhibits Akt and mTOR pathway activity. RU-SKI 43 hydrochloride demonstrates promising anti-cancer effects, making it a valuable tool for research in cancer biology and targeted therapy.
