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Catalog No.
Product Name
Application
Product Information
Citations
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CDK8 Inhibitor
CDK8-IN-11 is a potent and selective inhibitor of cyclin-dependent kinase 8 (CDK8), displaying an IC50 value of 46 nM. This compound effectively inhibits the WNT/β-catenin signaling pathway, making it a valuable tool for investigating the molecular mechanisms underlying oncogenesis. CDK8-IN-11 is primarily utilized in research related to colon cancer, contributing to the development of targeted therapeutic strategies. -
CDK6/9 Inhibitor
CDK6/9-IN-2 is a potent dual inhibitor of cyclin-dependent kinases CDK6 and CDK9, with reported IC50 values of 15 nM and 22 nM, respectively. This compound exhibits selectivity for CDK2, CDK8, and CDK11. CDK6/9-IN-2 effectively inhibits the proliferation of HaCaT cells stimulated by IFN-γ and TNF-α, while also suppressing the STAT3 signaling pathway and the expression of inflammatory factors. Its ability to alleviate psoriatic dermatitis makes CDK6/9-IN-2 valuable for research in psoriasis and related inflammatory conditions. -
KRAS Inhibitor
BBO-11818 is a highly selective non-covalent pan-KRAS inhibitor, targeting the Switch-II/Helix 3 pocket with an IC50 range of 28-120 nM. This compound effectively disrupts the KRAS:RAF1 interaction, leading to inhibition of the MAPK signaling pathway, resulting in significant anti-tumor effects. It demonstrates the ability to not only inhibit cell proliferation and induce apoptosis but also promote tumor regression in xenograft models. BBO-11818 is particularly valuable in research focused on KRAS mutation-related malignancies, including pancreatic cancer, non-small cell lung cancer, and colorectal cancer, and exhibits synergistic effects when used in combination with other therapeutic agents. -
CDK Inhibitor
AS2863619 free base is a selective inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), demonstrating IC50 values of 0.61 nM and 4.28 nM, respectively. This compound drives the conversion of antigen-specific effector and memory T cells into Foxp3+ regulatory T (Treg) cells, thereby offering potential therapeutic approaches for various immunological conditions. The inhibition of CDK8/19 by AS2863619 enhances STAT5 activation, leading to the upregulation of the Foxp3 gene and promoting Treg cell development. -
CDK3 Inhibitor
Vanicoside B is a potent inhibitor of cyclin-dependent kinase 8 (CDK8), derived from the herb Persicaria dissitiflora. This compound demonstrates significant anti-tumor activity by disrupting CDK8-mediated signaling pathways and reducing the levels of proteins associated with epithelial-mesenchymal transition. As a result, Vanicoside B induces cell cycle arrest and apoptosis, making it a valuable reagent for cancer research and therapeutic investigations targeting CDK8 pathways. -
ROCK2 Inhibitor
ROCK2-IN-12 is a selective ROCK2 inhibitor, demonstrating an IC50 of 7.0 nM for ROCK2 relative to ROCK1. This compound exhibits potent antifibrotic effects by modulating the TGF-β/Smad and ROCK2/STAT3 signaling pathways, effectively reducing collagen deposition and reversing fibrosis in Bleomycin-induced pulmonary fibrosis mouse models. ROCK2-IN-12 is suitable for investigating lung diseases, particularly pulmonary fibrosis. -
ROCK2 Inhibitor
ROCK2-IN-7 is a selective inhibitor of the Rho-associated protein kinase 2 (ROCK2). It effectively disrupts ROCK2/pSTAT3 signaling pathways, leading to decreased systemic immune activation and reduced inflammation. This compound is particularly valuable in studies related to autoimmune conditions, such as psoriasis, as it provides insights into the modulation of immune responses and inflammatory processes. -
CDK8/19 Inhibitor
CDK8/19-IN-2 is a potent and orally active inhibitor of cyclin-dependent kinases 8 and 19, exhibiting IC50 values of 2.08 nM and 2.49 nM, respectively. This compound is crucial for research focusing on acute myeloid leukemia (AML), breast cancer, and lymphoma, where inhibition of CDK8 and CDK19 can influence tumor proliferation and survival. Its selectivity and efficacy make it a valuable tool in studying the role of these kinases in various oncogenic pathways. -
PLK Inhibitor
Poloxipan is a pan-specific inhibitor targeting polo-like kinases (PLKs), specifically interfering with the Polo-box domain at the C-terminus. It demonstrates IC50 values of 3.2 μM, 1.7 μM, and 3.0 μM against PLK-1, PLK-2, and PLK-3, respectively. Additionally, Poloxipan inhibits various phospho-tyrosine binding domains, including the forkhead-associated domain of CHK-2 and the WW domain of peptidyl-prolyl cis/trans isomerase (PIN1). This compound is valuable for applications in cancer research, particularly in studies involving PLK pathways and associated cellular processes. -
CDK8/19 Inhibitor
CDK8-IN-16 is a potent dual inhibitor of cyclin-dependent kinases 8 and 19, demonstrating IC50 values of 5.1 nM and 5.6 nM, respectively. This compound effectively inhibits phospho-STAT1SER727 with an IC50 of 17.9 nM in SW620 cells and modulates the WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cells. CDK8-IN-16 exhibits favorable pharmacokinetic properties, including an oral bioavailability of 57% in rat models, making it a valuable tool for research in cancer biology and therapeutic development. -
KRAS G12D Inhibitor
KRAS G12D-IN-30 is a selective inhibitor of the KRAS G12D mutant, targeting the KRAS oncogene involved in various cancers. By inhibiting the activation of the downstream MAPK signaling cascade, specifically the Raf1-MEK-ERK pathway, this compound provides valuable insights into oncogenic signaling mechanisms. KRAS G12D-IN-30 is suitable for cancer research applications, particularly in studies focusing on KRAS-driven tumor biology and therapeutic strategies. -
KRAS Inhibitor
KRAS inhibitor-27 is a specific inhibitor targeting KRAS mutations, particularly effective against KRAS G12D and G12V variants. It demonstrates potent biological activity with IC50 values of 378 nM and 0.6 nM in AsPC-1 and SW620 cell lines, respectively, while showing a markedly reduced effect on wildtype KRAS HT-29 cells (IC50 3230 nM). This compound effectively inhibits ERK phosphorylation and reduces DUSP4 expression, thereby disrupting the MAPK signaling pathway. KRAS inhibitor-27 is valuable for research applications focusing on cancer biology and therapeutic strategies against KRAS-driven tumors. -
CDK9/FLT3 Inhibitor
CDDD11-8 is a potent and selective inhibitor of cyclin-dependent kinase 9 (CDK9) and FLT3-ITD, exhibiting Ki values of 8 nM and 13 nM, respectively. This compound effectively reduces the proliferation of leukemia cell lines, particularly those associated with the FLT3-ITD mutation. CDDD11-8 serves as a valuable tool for research into targeted therapies for hematological malignancies, specifically in the study of cell cycle regulation and tyrosine kinase signaling pathways. -
Dual FLT3/CHK1 Inhibitor
FLT3/CHK1-IN-1 is a dual inhibitor targeting both FLT3 and CHK1, demonstrating significant selectivity for c-KIT over other kinases. With an IC50 value of 58.4 μM, it shows reduced affinity for the hERG channel, minimizing potential cardiac side effects. FLT3/CHK1-IN-1 has exhibited efficacy in inhibiting tumor growth in mouse xenotransplantation models with MV-4-11 cells, making it a valuable tool for cancer research and therapeutic development. -
FLT3/CDK5 Inhibitor
AMG 925 (HCl) is a potent dual inhibitor targeting FLT3 and CDK5, demonstrating IC50 values of 2±1 nM and 3±1 nM, respectively. This compound exhibits selectivity for these kinases, making it a valuable tool for research into hematological malignancies and cancer progression. Its oral bioavailability further enhances its utility in preclinical studies investigating therapeutic interventions for FLT3-driven malignancies and CDK5-associated diseases. -
FLT3/CDK4 Inhibitor
FLT3/CDK4-IN-1 is a highly selective, orally active dual inhibitor targeting FLT3 and CDK4, demonstrating IC50 values of 11 nM and 7 nM, respectively. This compound exhibits significant antiproliferative activity against specific cancer cell lines and shows promising antitumor effects in vivo. FLT3/CDK4-IN-1 is suitable for research applications focused on cancer biology, particularly in exploring pathways associated with leukemias and solid tumors. -
PLK4 Inhibitor
CZS-241 is a selective Polo-like Kinase 4 (PLK4) inhibitor, exhibiting an IC50 of 2.6 nM. In addition to its primary activity, CZS-241 also inhibits TRKA with an IC50 of 2.74 μM. This compound induces apoptosis and effectively arrests the cell cycle at the S/G2 phase. CZS-241 demonstrates potent antiproliferative effects against leukemia cell lines while maintaining safety profiles in normal cell lines, making it a valuable tool for cancer research. -
CDK Inhibitor
(E/Z)-SU9516 is a selective inhibitor of cyclin-dependent kinases (CDKs), primarily targeting CDK2, with an IC50 value of 22 nM. This compound also exhibits inhibitory effects on CDK1 and CDK4, with IC50 values of 40 nM and 200 nM, respectively. Its potent inhibition of CDKs makes (E/Z)-SU9516 a valuable tool for studying cell cycle regulation and therapeutic applications in cancer research. -
c-Myc Inhibitor
Y502-3888 is a selective c-Myc inhibitor that targets the G-quadruplex (G4) structure of c-Myc, effectively impairing its transcriptional activity. This compound downregulates c-Myc expression at both mRNA and protein levels, leading to reduced viability and induced apoptosis in myeloma cells. Y502-3888 serves as a valuable tool for investigating the role of c-Myc in multiple myeloma and other related malignancies. -
CDK4 Inhibitor
3-ATA is a selective inhibitor of cyclin-dependent kinase 4 (CDK4), demonstrating both neuroprotective and antitumor properties. This compound has been shown to reduce kainic acid-induced apoptosis in cerebellar granule neurons, making it a valuable tool for investigating neurodegenerative diseases. Its ability to modulate cell cycle progression and prevent neuronal death highlights its potential applications in both cancer research and neuroprotection studies. -
CDK9-Cyclin T1 PPI Inhibitor
CDK9-Cyclin T1 PPI-IN-1 is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction. This compound effectively inhibits cell proliferation in triple-negative breast cancer (TNBC) MDA-MB-231 cells with an IC50 of 0.044 μM and promotes apoptosis. Additionally, CDK9-Cyclin T1 PPI-IN-1 suppresses CDK9 transcriptional activity and diminishes the phosphorylation of RNA Polymerase II at the CTD serine 2 residue. In vivo studies further demonstrate its capability to inhibit tumor growth in a TNBC 4T1 mouse model. -
CDK Inhibitor
CDK-IN-9 is a potent cyclin-dependent kinase (CDK) inhibitor that serves as a molecular glue, promoting the interaction between CDK12 and DDB1. With an IC50 value of 4 nM for CDK2/E, CDK-IN-9 facilitates the polyubiquitination and subsequent degradation of cyclin K. Additionally, it induces apoptosis through the dephosphorylation of retinoblastoma protein and RNA polymerase II, making it a valuable tool for research in cancer biology and cell cycle regulation. -
CDK4/CDK6 Inhibitor
CDK4/6-IN-10 is a potent and selective inhibitor of CDK4 and CDK6, exhibiting IC50 values of 22 nM and 10 nM, respectively. This compound demonstrates significant antitumor activity and is particularly relevant for research targeting multiple myeloma (MM). Its oral bioavailability combined with its selectivity makes CDK4/6-IN-10 a valuable tool for investigating the therapeutic potential in cancer biology. -
PARP1/2/CDK12 Inhibitor
PARP-1/2-IN-2 is a potent inhibitor of PARP1, PARP2, and CDK12, exhibiting IC50 values of 34 nM, 30 nM, and 285 nM, respectively. This compound disrupts DNA damage repair mechanisms, leading to induced cell cycle arrest and apoptosis. Notable for its efficacy in targeted therapy, PARP-1/2-IN-2 effectively inhibits the growth of triple-negative breast cancer (TNBC) cells and demonstrates significant antitumor activity in TNBC xenograft models. This makes it a valuable tool for research in cancer biology and therapeutic development. -
Aurora-A kinase Inhibitor
LY3295668 erbumine is a potent and selective inhibitor of Aurora-A kinase, exhibiting a Ki value of 0.8 nM for AurA while demonstrating significantly lower binding affinity for AurB at 1038 nM. This compound effectively inhibits the autophosphorylation of Aurora-A, leading to mitotic arrest and apoptosis without promoting polyploidy associated with AurB inhibition. LY3295668 erbumine is valuable for research into small cell lung cancer and other conditions involving dysregulation of Aurora kinases. -
CDK1 Inhibitor
Avotaciclib sulfate is an orally bioavailable inhibitor of cyclin-dependent kinase 1 (CDK1). It effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. This compound is particularly useful for research applications focused on oncology, including the study of pancreatic and lung cancer. -
c-Myc G4 Inhibitor
c-Myc inhibitor 16 iodide is a selective inhibitor of the c-Myc G-quadruplex, effectively targeting the c-Myc gene's transcription and translation processes. It disrupts the tumor cell cycle by arresting growth in the G0/G1 phase and activates the mitochondrial apoptosis pathway, leading to early apoptosis in cancer cells. This compound has significant potential in research applications related to breast cancer. -
Aurora B Inhibitor
HOI-07 is a selective inhibitor of Aurora B kinase that interferes with the phosphorylation of histone H3 at Ser10 in lung cancer cells. This compound induces cell-cycle arrest and apoptosis, demonstrating significant antitumor activity. HOI-07 effectively suppresses tumor growth in xenograft models, including A549, 143B, and KHOS, making it a valuable tool for cancer research and therapeutic investigation. -
c-Myc Inhibitor
EP12 is a selective c-Myc inhibitor that stabilizes c-Myc G-quadruplexes. This compound induces apoptosis and causes DNA damage in multiple myeloma cells, effectively inhibiting their growth. Additionally, EP12 disrupts the nuclear translocation of P65/P50 by interfering with the NF-κB signaling pathway, highlighting its potential in cancer research and therapeutic applications. -
PKMYT1 Inhibitor
XH-30 is a potent and selective inhibitor of PKMYT1, exhibiting an IC50 of 4.1 nM. This compound effectively suppresses the proliferation of P53-mutated triple-negative breast cancer (TNBC) cells by promoting G2/M phase release, inducing DNA damage, and triggering apoptosis. Additionally, XH-30 demonstrates significant antitumor effects in MDA-MB-231 mouse models, making it a valuable tool for research focused on P53-mutated TNBC. -
CHK1 Inhibitor
CHK1-IN-12 is a potent and selective checkpoint kinase 1 (CHK1) inhibitor that exerts its effects by significantly reducing CHK1 phosphorylation activity, thereby disrupting the DNA damage response pathway. With an in vitro enzyme IC50 of up to 10 nM and a cellular IC50 of 50 nM, CHK1-IN-12 effectively induces cell cycle arrest and apoptosis in tumor cells. This compound holds potential for cancer research, particularly in studies focused on cell cycle regulation and DNA repair mechanisms. -
CDK12/CDK13 Inhibitor
ZSQ836 is an orally active dual covalent inhibitor of CDK12 and CDK13, demonstrating an EC50 value of 32 nM for CDK12 inhibition. This compound has been shown to induce apoptosis and exhibits significant anticancer efficacy in vivo. ZSQ836 is a valuable tool for investigating the mechanisms and treatment strategies associated with ovarian cancer. -
PLK1 Inhibitor
PLK1-IN-16 is a potent and selective inhibitor of polo-like kinase 1 (PLK1) with an IC50 value of 0.25 nM. This compound is primarily utilized in cancer research due to its ability to induce G2 phase cell cycle arrest and promote apoptosis, displaying significant antiproliferative activity against various tumor cell lines. Additionally, PLK1-IN-16 has been shown to exhibit stability under simulated gastric acid conditions and presents manageable CYP 450 inhibition. Its applications extend to the study of triple-negative breast cancer (TNBC), breast cancer, and leukemia. -
PLK4 Inhibitor
Ocifisertib hydrochloride is a potent inhibitor of Polo-like kinase 4 (PLK4) with a Ki value of 0.26 nM and an IC50 of 2.8 nM. This compound demonstrates significant biological activity by inhibiting the growth of various cancer cell lines, inducing cell cycle arrest at the G2/M phase, and promoting apoptosis. Research applications include evaluating its antitumor efficacy in preclinical models, making it a valuable reagent for studying mechanisms of cancer progression and potential therapeutic strategies. -
CHK1 Inhibitor
Prexasertib lactate is a selective ATP-competitive inhibitor of checkpoint kinase 1 (CHK1), with a Ki value of 0.9 nM and an IC50 of less than 1 nM. It also inhibits CHK2 and RSK1 with IC50 values of 8 nM and 9 nM, respectively. By inducing double-stranded DNA breaks and leading to replication catastrophe, Prexasertib lactate promotes apoptosis in cancer cells. Its potent anti-tumor efficacy makes it a valuable tool for cancer research and therapeutic development. -
c-Myc Inhibitor
(-)-CMLD010509 is a potent c-Myc inhibitor that selectively targets the oncogenic translation program associated with multiple myeloma. This compound demonstrates significant activity, exhibiting an IC50 of less than 10 nM in various multiple myeloma cell lines, leading to the induction of apoptosis. (-)-CMLD010509 operates through a mechanism that is independent of eIF4E phosphorylation, making it a valuable tool for studying the translation control of key oncoproteins such as MYC, MDM2, CCND1, MAF, and MCL-1. -
CDK Inhibitor
R547 mesylate is a potent and selective ATP-competitive inhibitor of cyclin-dependent kinases (CDKs). It exhibits inhibitory constants of 2 nM for CDK1/cyclin B, 3 nM for CDK2/cyclin E, and 1 nM for CDK4/cyclin D1. Due to its oral bioavailability and high specificity, R547 mesylate is valuable for investigating cell cycle regulation and the role of CDKs in cancer research. -
CDK Inhibitor
Otviciclib is a potent cyclin-dependent kinase (CDK) inhibitor that demonstrates significant anti-proliferative effects against various solid tumor cell lines, including HCT116, NCIH82, and DU145. This compound effectively induces cell cycle arrest in the G2/M phase and triggers apoptosis, exhibiting a favorable toxicity profile towards normal cells. Otviciclib shows broad-spectrum anticancer activity, making it a valuable tool for research applications related to colon, pancreatic, and lung cancers. -
Aurora Kinase Inhibitor
Aurora Kinase Inhibitor-14 is a highly selective inhibitor of Aurora kinases, demonstrating IC50 values of 0.5 nM for Aurora A and 1.2 nM for Aurora B. This compound binds to the ATP-binding site of these kinases, effectively disrupting chromosome segregation during mitosis and promoting apoptosis in tumor cells. Aurora Kinase Inhibitor-14 is a valuable tool for investigating the therapeutic potential in various solid tumors and hematological malignancies, including non-small cell lung cancer, breast cancer, and acute myeloid leukemia. -
DYRK1A/DYRK1B Inhibitor
JH-XVII-10 is a highly selective inhibitor of DYRK1A and DYRK1B, exhibiting IC50 values of 3 nM and 5 nM, respectively. This compound demonstrates significant antitumor activity in head and neck squamous cell carcinoma (HNSCC) cell lines. JH-XVII-10 is suitable for research applications focusing on dysregulation of DYRK kinases in cancer. -
Wee1/HDAC Inhibitor
Wee1/HDAC-IN-1 is a dual inhibitor targeting Wee1 and histone deacetylases (HDACs). It demonstrates potent activity with an IC50 of 1.2 nM for Wee1 and varying IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. This compound displays significant antiproliferative effects in MV4-11 cells, with an IC50 of 0.076 μM, by disrupting DNA damage repair mechanisms and promoting apoptosis. Wee1/HDAC-IN-1 is suited for research on acute myeloid leukemia (AML). -
CDK9/HDAC Dual Inhibitor
CDK9/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDACs. With IC50 values of 0.17 μM for CDK9, 1.73 μM for HDAC1, and 1.11 μM for HDAC3, this compound effectively disrupts the activity of these proteins. It induces cancer cell apoptosis and causes cell cycle arrest at the G2/M phase. Additionally, CDK9/HDAC1/HDAC3-IN-1 exhibits broad-spectrum anti-cancer effects, demonstrating efficacy against various malignancies, including breast, cervical, and liver cancers, as evidenced in murine TNBC MDA-MB-231 xenograft models. -
CDK2 Inhibitor
CDK2-IN-9 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2), exhibiting an IC50 of 0.63 µM. This compound demonstrates significant antiproliferative activity, inducing apoptosis and causing cell cycle arrest at the S and G2/M phases. CDK2-IN-9 is suitable for research applications focused on melanoma and the exploration of CDK2's role in cell cycle regulation and cancer biology. -
Aurora A Inhibitor
Aurora A Inhibitor 2 is a potent inhibitor of Aurora A kinase, exhibiting an IC50 value of 21.94 nM. This compound has been shown to induce caspase-dependent apoptosis in MDA-MB-231 cells, highlighting its potential as a therapeutic agent in cancer research. It is useful for studies investigating the role of Aurora A in cell cycle regulation and apoptosis. -
CDKs Inhibitor
(Rac)-Roscovitine is a selective inhibitor of cyclin-dependent kinases (CDKs), functioning by competitively binding to their active sites in place of ATP. This mechanism effectively inhibits CDK phosphorylation activity, leading to apoptosis in cancer cells. As a valuable research tool, (Rac)-Roscovitine is applicable in studies of cancer and various conditions associated with CDK dysregulation, including neurodegenerative diseases, cardiac disorders, and chronic inflammation. -
HDAC/CDK Inhibitor
CDK/HDAC-IN-2 is a dual inhibitor of histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs), exhibiting IC50 values of 6.4 nM for HDAC1, 0.25 nM for HDAC2, 45 nM for HDAC3, and >1000 nM for HDAC6,8, as well as 8.63 nM for CDK1, 0.30 nM for CDK2, and >1000 nM for CDK4,6,7. This compound demonstrates significant antiproliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. CDK/HDAC-IN-2 is particularly valuable in cancer research due to its potent antitumor efficacy. -
CDK9 Inhibitor
CDK9-IN-18 is a selective inhibitor of cyclin-dependent kinase 9 (CDK9), effectively obstructing its phosphorylation activity. This compound demonstrates significant anticancer properties, promoting apoptosis in various cancer cell lines while exhibiting low cellular toxicity. Its mechanism of action makes CDK9-IN-18 a valuable tool for research into cancer therapeutics and the regulation of gene expression. -
CDK2/Topo I Inhibitor
ZLHQ-5f is a dual inhibitor of Cyclin-dependent kinase 2 (CDK2) and Topoisomerase I (Topo I), exhibiting an IC50 of 0.145 μM against CDK2/CycA2. This compound effectively induces S-phase cell cycle arrest and triggers apoptosis in HCT116 cancer cells. Its favorable safety profile supports its potential applications in cancer research and therapeutic development. -
CDK2/9 Inhibitor
CDK2/9-IN-1 is an orally active dual inhibitor targeting cyclin-dependent kinases CDK2 and CDK9, with IC50 values of 0.004 μM and 0.009 μM, respectively. This compound induces apoptosis through G2/M cell cycle arrest, demonstrating notable antitumor activity. CDK2/9-IN-1 is useful for research applications focused on cancer biology and the modulation of cell cycle regulation. -
Dual PLK1/BET Inhibitor
WNY0824 is a dual inhibitor targeting Polo-like kinase 1 (PLK1) and the Bromodomain and Extra-Terminal (BET) protein family. It demonstrates potent inhibitory activity, with IC50 values of 22 nmol/L for PLK1 and varying efficacy against BRD2, BRD3, BRD4, and BRDT. WNY0824 induces cell cycle arrest and apoptosis by disrupting AR- and MYC-mediated transcriptional processes, making it valuable for research in cancer biology. Furthermore, it has shown effectiveness in inhibiting tumor growth in Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenograft models, highlighting its potential in overcoming treatment resistance.
