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Catalog No.
Product Name
Application
Product Information
Citations
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K-Ras(G12C) inhibitor
K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C). -
Ras inhibitor
Antineoplaston A 10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer. -
pan-RAS inhibitor
Ras-IN-3144 is a pan-RAS inhibitor which inhibits RAS signaling pathways in cancer cells and prevents the growth of RAS mutant mouse cancer xenografts. -
ATP-competitive STK19 inhibitor
ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor. ZT-12-037-01 effectively blocks oncogenic NRAS-driven melanocyte malignant transformation and melanoma growth in vitro and in vivo. -
KRAS G12C inhibitor
KRAS G12C inhibitor 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM. -
KRAS G12C inhibitor
KRAS G12C inhibitor 16 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 39, has an IC50 of 97 nM. -
KRAS G12C inhibitor
KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM. -
KSR/Ras inhibitor
APS-2-79 HCl, small molecule that stabilizes the KSR (Kinase suppressor of Ras) inactive state and antagonizes oncogenic Ras signalling (IC50 value 120 nM against ATP-biotin probe-labelling of KSR2). -
KRAS G12C inhibitor
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity.
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GGTase I inhibitor
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM. -
SRE activation inhibitor
CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM. -
Rac1 inhibitor
1A-116 is a specific Rac1 inhibitor, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo.
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K-Ras inhibitor
K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.(the detailed information refer to the reference). -
K-ras G12C inhibitor
K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C. -
covalent K-Ras G12C inhibitor
K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor. -
K-ras G12C inhibitor
K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1. -
Epac inhibitor
EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 ?M in Swiss 3T3 cells. -
KRAS G12C covalent inhibitor
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. -
KRas G12C inhibitor
KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147. -
KRAS G12C covalent inhibitor
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity. -
KRAS G12C inhibitor
KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30. -
osteoclastic bone resorption inhibitor
Zoledronic acid is a bisphosphonate which used to multiple myeloma and prostate cancer treament. -
KRAS Inhibitor
KRAS inhibitor-9 is a selective inhibitor of the KRAS protein, primarily targeting KRAS G12D, G12C, and Q61H mutations with a moderate binding affinity (Kd=92 μM). This compound effectively disrupts the formation of the GTP-bound active form of KRAS, leading to subsequent inactivation of downstream signaling pathways. Biological assays demonstrate that KRAS inhibitor-9 induces G2/M cell cycle arrest and promotes apoptosis in non-small cell lung cancer (NSCLC) cells harboring KRAS mutations, while sparing normal lung cells. Its application is significant in cancer research, particularly in studying KRAS-driven malignancies. -
KRAS G12D Inhibitor
KRAS G12D inhibitor 14 is a selective inhibitor targeting the KRAS G12D mutation, exhibiting a binding affinity (KD) of 33 nM. This compound effectively reduces the levels of active KRAS G12D (KRAS G12D-GTP) without impacting the KRAS G13D variant. It is a valuable tool for research applications focused on elucidating the role of KRAS G12D in oncogenic signaling pathways and developing targeted cancer therapies. -
KRAS G12C Inhibitor
KRAS G12C-IN-76 is a selective inhibitor of the KRAS G12C mutation, a prominent driver in various cancers. This compound effectively reduces ERK phosphorylation, thereby impeding signaling pathways involved in tumor growth and proliferation. KRAS G12C-IN-76 demonstrates significant anti-cancer activity, particularly in pancreatic cancer models, making it a valuable tool for research in targeted therapies and cancer biology. -
KRas G12V Inhibitor
KRAS-IN-51 is a selective inhibitor of the KRas G12V mutant, exhibiting an IC50 of 2.9 nM. It demonstrates effective inhibition of pERK phosphorylation and shows significant anti-proliferative activity in colorectal cancer (SW620) and pancreatic cancer (MIAPaCa-2) cell lines. This compound is valuable for research focused on KRas-driven malignancies, contributing to the understanding of therapeutic strategies targeting KRas mutations. -
KRAS G12C Inhibitor
KRAS G12C Inhibitor 61 is a selective inhibitor targeting the KRAS G12C mutation. It effectively inhibits phospho-ERK 1/2 in MIA PaCa-2 cells, exhibiting an IC50 of 9 nM. This compound is valuable for research into pancreatic, colorectal, and lung cancers, contributing to studies focused on therapeutic strategies for KRAS-driven malignancies. -
KRAS(Q61H) Inhibitor
RM-046 is a selective inhibitor targeting the KRAS(Q61H) mutant, functioning through the formation of a ternary complex with cyclophilin A. This compound non-covalently binds to activated KRASQ61H, obstructing effector binding and thereby inhibiting downstream signal transduction pathways. RM-046 has demonstrated efficacy in suppressing ERK phosphorylation, stalling cancer cell proliferation, and promoting anti-tumor activity, including tumor regression in preclinical xenograft studies. It serves as a valuable tool for investigating KRASQ61H-associated malignancies. -
KRAS G12D Inhibitor
KRAS G12D-IN-27 is a selective inhibitor targeting the KRAS G12D mutant protein. It effectively inhibits ERK phosphorylation, exhibiting an IC50 of 112 nM. This compound is valuable for cancer research, particularly in studies focused on the KRAS signaling pathway and downstream effects in tumor biology. -
KRASG12C Inhibitor
KRASG12C IN-15 is a potent inhibitor of the KRASG12C mutation, functioning primarily by obstructing the SOS1-mediated GDP/GTP exchange, with an IC50 of 19 nM. It effectively inhibits ERK phosphorylation with an IC50 of 0.051 μM and demonstrates significant anti-proliferative effects on KRASG12C-mutated MIA PaCa-2 cells, with an IC50 of 0.023 μM. In vivo studies reveal that KRASG12C IN-15 exhibits notable antitumor efficacy in MIA PaCa-2 xenograft mouse models. This compound is valuable for investigating KRASG12C-associated signaling pathways and developing targeted therapies. -
KRAS Inhibitor
KRAS G12D inhibitor 25 selectively targets the KRAS G12D mutation and HSP90α, exhibiting IC50 values of less than 0.1 μM and between 0.1-1 μM, respectively. This compound effectively inhibits the proliferation of MIA PaCa-2 and NCI-H358 cell lines, displaying EC50 values of less than 0.1 μM and between 0.1-1 μM, respectively. Additionally, KRAS G12D inhibitor 25 promotes the degradation of ERBB2 with a DC50 range of 0.1-1 μM, making it a valuable tool for cancer research focusing on KRAS-targeted therapies. -
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.
