Catalog No.
Product Name
Application
Product Information
Citations
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Wee1 Inhibitor
PKMYT1-IN-4 is a potent PKMYT1 inhibitor with an IC50 of less than 50 nM. This compound selectively targets the Wee1 kinase, a critical regulator of the cell cycle. PKMYT1-IN-4 is utilized in research applications focused on cell cycle regulation and cancer biology, making it suitable for studies exploring therapeutic strategies against proliferative diseases. -
MYT1 Kinase Inhibitor
Myt1-IN-6 is a selective inhibitor of MYT1 kinase, which plays a crucial role in the regulation of cell cycle progression and neuronal differentiation. This compound is particularly relevant for studies involving RB1-deficient cancers, such as triple-negative breast cancer, where MYT1 activity may contribute to oncogenesis and tumor progression. Myt1-IN-6 serves as a valuable tool for exploring therapeutic strategies targeting MYT1 in various malignancies. -
G-quadruplex Inhibitor
Phen-DC3 Trifluoromethanesulfonate is a specific ligand that targets G-quadruplex (G4) structures, effectively inhibiting the helicases FANCJ and DinG with IC50 values of 65±6 nM and 50±10 nM, respectively. This compound plays a critical role in research focused on telomere biology, DNA replication, and cancer therapeutics. Its ability to modulate G4 structures makes it a valuable tool for investigating G4-associated cellular processes and the development of novel anti-cancer strategies. -
G-quadruplex Ligand
Carboxy pyridostatin trifluoroacetate salt is a G-quadruplex ligand that selectively interacts with G-quadruplex structures in RNA and DNA. This compound has been shown to decrease levels of ATF-5 protein, thereby inhibiting cell proliferation and disrupting stress granule formation. It serves as a valuable tool in the study of G-quadruplex biology and its implications in cellular stress responses and cancer research. -
G-quadruplex Stabilizer
BMVC2 is a bisubstituted carbazole derivative that serves as a G-quadruplex (G4) stabilizer. This compound promotes the formation and stabilization of G-quadruplex structures, which are important in the regulation of gene expression and telomere maintenance. BMVC2 is utilized in research applications focusing on cancer biology, antiviral therapies, and the development of novel molecular therapeutics targeting G4 DNA structures. -
G-quadruplex Ligand
Carboxypyridostatin is a selective ligand for G-quadruplex structures. It demonstrates significant affinity for RNA G-quadruplexes, leading to the downregulation of ATF-5 protein levels. This compound is known to inhibit cell proliferation and interfere with stress granule formation, making it valuable for studies on cellular stress responses and G-quadruplex-related mechanisms in cancer research. -
G-quadruplexes Stabilizer
Pyridostatin trihydrochloride is a potent G-quadruplex stabilizer with a binding affinity (Kd) of 490 nM, effectively targeting DNA and RNA G-quadruplex structures within cellular environments. This compound induces growth arrest in human cancer cells through mechanisms involving replication- and transcription-dependent DNA damage. Pyridostatin specifically impacts the proto-oncogene Src, leading to diminished SRC protein levels and reduced SRC-dependent cellular motility in human breast cancer cells. Its applications extend to cancer research, particularly in studying mechanisms of tumor progression and drug resistance. -
G-quadruplex
Nemorubicin hydrochloride is a doxorubicin derivative that primarily targets G-quadruplex structures. It exhibits notable antitumor activity by intercalating into duplex DNA while also serving as a potent ligand for G-quadruplex DNA segments, effectively stabilizing their conformation. This compound is valuable for research applications focused on understanding G-quadruplex biology and developing therapeutic strategies targeting this unique DNA structure. -
LIMK Inhibitor
CRT0105950 is a potent LIMK inhibitor, selectively targeting LIMK1 and LIMK2 with IC50 values of 0.3 nM and 1 nM, respectively. Its primary mechanism involves the inhibition of LIM kinases, which play a crucial role in regulating actin cytoskeleton dynamics and cell motility. This reagent is valuable for investigating tumor biology and potential therapeutic pathways in cancer research. -
LIMK1 Inhibitor
SR7826 is a potent and selective LIMK1 inhibitor, exhibiting an IC50 of 43 nM. This bis-aryl urea derivative demonstrates over 100-fold selectivity for LIMK1 compared to ROCK and JNK kinases. SR7826 serves as a valuable tool for investigating LIMK1-related signaling pathways and its role in cellular processes such as cytoskeletal dynamics and cancer progression. -
LIMK1/2 Inhibitor
TH470 is a highly selective inhibitor of LIMK1 and LIMK2, exhibiting IC50 values of 9.8 nM and 13 nM, respectively. This compound effectively modulates the actin cytoskeleton and related cellular processes by inhibiting LIM kinase activity. TH470 is particularly valuable in the study of orphan diseases and other conditions related to dysregulated LIMK signaling. -
LIMK Inhibitor
LIMK1 inhibitor BMS-4 is a selective inhibitor of LIM Kinases (LIMK1 and LIMK2). By inhibiting LIMK1, BMS-4 effectively blocks the phosphorylation of cofilin, a critical substrate, thereby modulating actin dynamics. It has demonstrated noncytotoxicity in A549 cells, making it a valuable tool for investigating LIMK-related pathways and their roles in cancer cell migration and invasion. -
LIM Kinase (LIMK) Inhibitor
MDI-114215 is an allosteric inhibitor targeting LIM Kinase 1 and 2 (LIMK1/2). It effectively inhibits the phosphorylation of cofilin in induced pluripotent stem cells (iPSCs) derived from mouse brain regions. This compound shows potential applications in research related to Fragile X Syndrome (FXS), enabling investigations into cellular pathways affected by LIMK activity. -
LIMK1 Inhibitor
LIMK1 inhibitor 2 is a selective inhibitor of LIM kinase 1 (LIMK1), demonstrating an IC50 value of 9 μM. This compound effectively blocks LIMK1 activity, leading to the modulation of cytoskeletal dynamics. It is primarily utilized in research to investigate cellular processes such as cell migration, proliferation, and differentiation, contributing valuable insights into cancer biology and other related fields. -
LIMK1 Inhibitor
8β,9α-Dihydroxylindan-4(5),7(11)-dien-8alpha,12-olide is a sesquiterpene that acts as a selective inhibitor of LIMK1. By targeting this kinase, the compound effectively modulates cell motility, making it valuable for studies investigating cytoskeletal dynamics and cell migration. This reagent is applicable in various research contexts, including cancer metastasis and neurobiology, where LIMK1 plays a critical role. -
LIMK2 Inhibitor
LIMK-IN-3 is a potent inhibitor of LIMK2, demonstrating an IC50 of 1.2 nM. This compound exhibits significant inhibition of LIMK2 activity, which is crucial for understanding the role of LIMK2 in various cellular processes. LIMK-IN-3 is particularly relevant in glaucoma research, providing valuable insights into the molecular mechanisms underlying this condition. -
LIMK Inhibitor
LIJTF500025 is a potent and selective LIMK inhibitor that targets LIMK1 and LIMK2, exhibiting pIC50 values of 6.77 and 7.03, respectively, as determined by NanoBRET. This compound plays a crucial role in modulating actin dynamics and has potential applications in cancer research. Its ability to inhibit LIM kinase activity makes it a valuable tool for investigating the mechanisms underlying tumor progression and metastasis. -
LIMK1 Inhibitor
CRT 0105446 is a selective inhibitor of LIMK1, exhibiting an IC50 value of 8 nM. This compound is valuable for investigating the role of LIMK1 in cellular processes such as cytoskeletal dynamics and cell migration. Researchers can utilize CRT 0105446 to explore its effects in studies related to cancer, neurodegenerative diseases, and other conditions where LIMK1 modulation is implicated. -
LIM1 Inhibitor
Curcolonol is a furan-type sesquiterpene that acts as an inhibitor of LIM kinase 1. It exhibits significant inhibitory activity against this target, making it a valuable compound for studying pathways involved in cancer progression. Curcolonol is particularly relevant for research applications in breast cancer, providing insights into potential therapeutic mechanisms and treatment strategies. -
LIMK Inhibitor
LIMK-IN-2 is a selective LIMK inhibitor that exhibits significant capacity to inhibit cell migration in osteosarcoma and cervical cancer cells. This compound demonstrates potential anti-angiogenic activity, making it a valuable tool for investigating the role of LIMK in cancer progression and therapeutic strategies. Research applications include studies focused on metastasis and the regulation of cellular motility in tumor biology. -
LIMK1 Inhibitor
LIMK1 Inhibitor 1 is a selective inhibitor of LIM domain kinase 1 (LIMK1), a critical regulator of actin cytoskeletal dynamics. This compound demonstrates potential anti-cancer activity by disrupting cancer cell migration and invasion. LIMK1 Inhibitor 1 is applicable in research focused on understanding the role of LIMK1 in oncogenesis and exploring therapeutic strategies for cancer treatment. -
PLK-1/Tubulin Inhibitor
3,4,3'-Tri-O-methylflavellagic acid is a flavonoid compound that functions as an inhibitor of polo-like kinase-1 (PLK-1) and αβ-tubulin at the colchicine binding site. This compound disrupts microtubule assembly dynamics and modulates kinase activity, making it valuable for research into cancer cell proliferation and anti-nociceptive properties. Its unique biological activities make it a significant reagent for studies focused on cancer therapies and pain management. -
TTK/PLK1 Inhibitor
TTK/PLK1-IN-1 is a potent inhibitor of threonine tyrosine kinase (TTK) and polo-like kinase 1 (PLK1), demonstrating IC50 values of 7 nM and 72 nM, respectively. This compound plays a crucial role in regulating the spindle assembly checkpoint (SAC), making it relevant for cancer research. It exhibits promising antitumor activity against triple-negative breast cancer (TNBC), contributing to its potential applications in oncology studies. -
PLK1 Inhibitor
GSK461364 analogue 1 is a thiophene-based inhibitor targeting Polo-like kinase 1 (PLK1), exhibiting an IC50 value of 2 nM, along with inhibitory activity against PLK3 (IC50: 630 nM) and Nek2 kinase (IC50: 21 nM). With a solubility of ≥190 μM in pH 7.4 PBS and a human plasma protein binding rate of 91.5%, this compound is suitable for in vitro studies. GSK461364 analogue 1 is particularly relevant for research into malignancies such as colon, lung, breast, and ovarian cancers. -
pan-KRAS Inhibitor
Eras-4001 is a pan-KRAS inhibitor that demonstrates significant antitumor activity by effectively inhibiting the proliferation of both wild-type and mutant KRAS cancer cells, including variants such as KRASG12D, KRASG12V, and KRASG12C. In preclinical studies, Eras-4001 has evidenced a robust ability to suppress tumor growth in xenograft mouse models, such as GP2D and Panc0403, making it a valuable tool for investigating KRAS-driven malignancies and potential therapeutic strategies in cancer research. -
KRAS Agonist
KRA-533 is a potent KRAS agonist that selectively binds to the GTP/GDP binding pocket of the KRAS protein. This interaction inhibits GTP cleavage, leading to the accumulation of constitutively active GTP-bound KRAS. Consequently, KRA-533 induces both apoptotic and autophagic cell death pathways in cancer cells, making it a valuable tool for research into cancer biology and therapeutic strategies targeting KRAS signaling. -
Cdc42 Inhibitor
CID44216842 is a selective inhibitor of the small GTPase Cdc42, acting primarily by disrupting its guanine nucleotide binding. It demonstrates potent inhibitory activity with EC50 values of 1.0 μM and 1.2 μM for wild-type Cdc42 and the Cdc42Q61L mutant, respectively, in GTP binding assays, and 0.3 μM and 0.5 μM in GDP binding assays. This compound is suitable for use as a molecular probe in studies related to Cdc42 signaling pathways and its role in cellular processes such as cytoskeletal dynamics and cell migration. -
KRAS G12D Inhibitor
AZD0022 is a selective and orally active inhibitor of the KRAS G12D mutant protein. It effectively disrupts the KRAS signaling pathway, demonstrating suppression of tumor growth in the GP2D xenograft model. This compound is relevant for research in cancer therapeutics, particularly for investigating KRAS-driven malignancies. -
KRAS Inhibitor
KRAS inhibitor-3 is a selective inhibitor of the KRAS protein, effectively targeting both wild-type and various oncogenic mutants, including KRAS G12C, G12D, and Q61H, with affinities ranging from 0.28 μM to 0.74 μM. This compound disrupts the interaction between KRAS and Raf, thereby influencing downstream signaling pathways critical for cell proliferation and survival. KRAS inhibitor-3 is a valuable tool for research applications focused on cancer biology and the development of targeted therapies for KRAS-driven malignancies. -
Cdc42/Rac1 Inhibitor
l-Naproxen is an enantiomer of (S)-Naproxen, functioning as an inhibitor of Cdc42 and Rac1 with EC50 values of 96 μM and 212 μM, respectively. It exhibits anti-tumor activity in addition to its role as a nonsteroidal anti-inflammatory drug (NSAID). This compound is valuable for research applications involving cellular signaling pathways, inflammation, and cancer biology. -
KRasG12C Inhibitor
CFL-137 is a potent inhibitor of KRasG12C, a pivotal mutation implicated in various cancers. This compound demonstrates significant antiproliferative activity, making it a valuable tool for studying oncogenic signaling pathways. CFL-137 holds promise for research applications focused on lung cancer and other KRas-driven malignancies. -
KRAS Inhibitor
KRAS Inhibitor-10 is a selective inhibitor targeting RAS proteins, with a strong emphasis on KRAS variants. This orally active compound demonstrates significant anti-cancer activity, making it suitable for research applications in various malignancies, including pancreatic cancer, breast cancer, multiple myeloma, leukemia, and lung cancer. KRAS Inhibitor-10 is derived from a tetrahydroisoquinoline structure and is detailed in patent WO2021005165 A1. -
KRASG12D Mutant Inhibitor
KRAS G12D-IN-29 is a selective inhibitor targeting the KRAS G12D mutant, known for its oral bioavailability. This compound effectively disrupts downstream signaling pathways associated with KRAS G12D, leading to a reduction in tumor cell proliferation. KRAS G12D-IN-29 shows potential for research applications focused on cancers driven by the KRAS G12D mutation, including pancreatic, lung, and colorectal cancers. -
KRAS Inhibitor
KRAS Inhibitor-31 is a potent inhibitor targeting mutant forms of the KRAS protein, specifically KRAS G12D, G12C, and G12V, with KD (SPR) values of 0.019 nM, 0.019 nM, and 0.096 nM, respectively. This compound demonstrates significant biological activity in the inhibition of KRAS-driven signaling pathways, making it a valuable tool for research in cancer biology, particularly in the study of tumors harboring KRAS mutations. -
pan-KRAS Inhibitor
pan-KRAS-IN-2 is a potent pan-KRAS inhibitor with IC50 values of ≤ 10 nM against both wild-type and prevalent mutant forms of KRAS, including G12D, G12C, G12V, G12S, G12A, and Q61H, while exhibiting an IC50 > 10 μM for KRAS G13D. This compound is valuable for investigating KRAS-mediated cancers, specifically in pancreatic and colorectal cancer models, aiding in the understanding of tumor biology and potential therapeutic interventions. -
EPAC1 Agonist
I942 is a selective non-cyclic nucleotide (NCN) agonist of EPAC1. It effectively modulates proinflammatory cytokine signaling pathways associated with various cardiovascular diseases. This compound serves as a valuable tool in research focused on understanding EPAC1-related mechanisms and developing therapeutic strategies for inflammatory cardiovascular conditions. -
Isomer
(R)-BI-2852 is the isomer of BI-2852, designed as an experimental control in KRAS research. It functions as a KRAS inhibitor targeting the switch I/II pocket with nanomolar affinity, displaying a ten-fold stronger binding to active KRASG12D compared to KRAS wild type. This compound effectively disrupts guanine nucleotide exchange factor, GTPase-activating protein, and effector interactions with KRAS, resulting in the inhibition of downstream signaling pathways and an antiproliferative effect in KRAS mutant cell lines. -
Rac1 Inhibitor
Rac1-IN-3 is an inhibitor of the Rac1 protein, exhibiting an IC50 of 46.1 μM. This compound effectively disrupts Rac1 signaling pathways, which are implicated in various cellular functions such as cytoskeletal dynamics and cell migration. Rac1-IN-3 is valuable for research applications focused on cancer biology, neurodegenerative diseases, and cardiovascular disorders, providing insights into the role of Rac1 in disease progression and therapeutic targeting. -
pan-KRAS Inhibitor
pan-KRAS-IN-18 is a pan-KRAS inhibitor targeting both KRAS wild-type and KRAS G12V, with IC50 values of 29 nM and 9 nM, respectively. This compound demonstrates significant antiproliferative activity in KRAS-mutant cell lines, making it a valuable tool for researchers studying KRAS-driven cancers. Its application is particularly relevant in the context of lung cancer research. -
KRAS G12C Inhibitor
Divarasib adipate is a potent and selective inhibitor of KRAS G12C with an IC50 of <0.01 μM. By covalently binding to the switch II pocket of KRAS G12C, Divarasib irreversibly stabilizes the protein in its inactive GDP-bound state. This compound is primarily utilized in research applications focused on cancer biology, particularly in studies targeting KRAS-driven tumors. -
KRAS(G12D) Inhibitor
MRTX-EX185 formic is a potent inhibitor of KRAS(G12D) with an IC50 of 90 nM. It effectively binds to both GDP-loaded and active GTP-bound states of KRAS, displaying broad-spectrum activity with additional IC50 values of 110, 290, 130, and 240 nM for KRAS WT, KRAS(G12C), KRAS(Q61H), and KRAS(G13D), respectively. MRTX-EX185 formic also shows affinity for GDP-loaded HRAS. This compound is valuable for investigating RAS-driven tumors, including pancreatic cancer, facilitating insights into therapeutic strategies targeting KRAS mutations. -
Pan-RAS Inhibitor
Pan-RAS-IN-3 is a pan-RAS inhibitor that targets various isoforms of the RAS protein family, known for their role in promoting cellular proliferation and survival. This compound exhibits significant biological activity in inhibiting the signaling pathways associated with melanoma and acute myeloid leukemia. It is a valuable tool for researchers investigating RAS-driven cancers and studying the therapeutic potential of targeting these oncogenic signaling pathways. -
KRAS Inhibitor
KRAS inhibitor-24 is a pyridopyrimidine compound that selectively inhibits KRAS with an IC50 of less than 100 nM for KRas G12V, KRas WT, and KRas G12R mutants. This compound demonstrates substantial biological activity in disrupting KRAS-mediated signaling pathways. KRAS inhibitor-24 is utilized in preclinical research to study KRAS-driven tumors and to investigate potential therapeutic strategies targeting KRAS mutations in various cancers. -
KRAS Inhibitor
(1R)-KRAS inhibitor-24 is a pyridopyrimidine compound that selectively inhibits KRAS, demonstrating an IC50 of less than 100 nM for KRas G12V, KRas Wild Type, and KRas G12R variants. This inhibitor serves as a valuable tool for research applications focused on KRAS-driven cancers, providing insights into signaling pathways and potential therapeutic modalities targeting this critical oncogene. -
KRAS G12D Inhibitor
KRAS G12D-IN-31 is a potent inhibitor of the KRAS G12D mutation, exhibiting an IC50 of less than 100 nM. It effectively inhibits the proliferation of RAS-dependent cancer cells, including those harboring KRAS G12C, KRAS G12D, KRAS G12V, and KRASWT. This compound is particularly valuable for research applications involving non-small cell lung cancer, gastric cancer, colon cancer, and malignant melanoma, facilitating the exploration of KRAS-targeted therapies. -
RAS Ligand
VVD-849 is a RAS ligand that covalently binds to Cys242 in the RAS-binding domain of PI3K p110α, facilitating the interaction between RAS and PI3K. This compound exhibits partial inhibition of pAKT (S473) specifically in HER2-overexpressing tumors. VVD-849 is utilized in cancer research, particularly for studying the mechanisms underlying breast cancer progression and RAS-related signaling pathways. -
KRAS(G12D) Inhibitor
TH-Z827 is a selective inhibitor of the KRAS(G12D) mutant, demonstrating an IC50 of 2.4 μM. This compound does not interact with wild-type KRAS or the KRAS(G12C) variant. TH-Z827 effectively disrupts the interaction between KRAS(G12D) and CRAF, with an IC50 value of 42 μM, making it a valuable tool for studying KRAS-driven cancers and developing targeted therapies. -
KRAS G12D Inhibitor
KRAS G12D Inhibitor 3 TFA is a selective inhibitor targeting the KRAS G12D mutation, exhibiting an IC50 of less than 500 nM. This compound demonstrates significant antitumor activity, making it a valuable tool in cancer research related to KRAS-driven malignancies. Additionally, KRAS G12D Inhibitor 3 TFA features an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), thus facilitating the development of bioconjugates and other applications in chemical biology. -
Lbc-RhoA Interaction Inhibitor
(E/Z)-ZINC09659342 is a potent inhibitor of the Lbc-RhoA protein interaction, impacting RhoA-mediated cellular signaling pathways. This compound is valuable for studies focused on RhoA's role in cell adhesion, migration, and cytoskeletal dynamics. It serves as a useful tool for researchers investigating the molecular mechanisms of various diseases associated with RhoA dysregulation. -
KRAS G12C Inhibitor
KRAS G12C inhibitor 14 is a potent inhibitor specifically targeting the KRAS G12C mutation, with an IC50 value of 18 nM. This compound effectively disrupts the activity of the KRAS protein, making it a valuable tool for studies on cancer biology, particularly in models of tumors driven by KRAS mutations. Its application extends to drug discovery and development efforts aimed at novel therapeutic strategies for KRAS-driven malignancies.
