- Cat. No.
- A16097
6H05
Synonyms: K-Ras inhibitor
6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
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Ras inhibitors and related small GTPase modulators act on KRAS and on the Rac, Rho and Cdc42 proteins. Small GTPases of the Ras superfamily work as molecular switches. They cycle between an active form bound to guanosine triphosphate (GTP) and an inactive form bound to guanosine diphosphate (GDP). Oncogenic KRAS mutations such as G12C keep the protein in its signaling state. ARS-853 and KRas G12C inhibitor 4 target the mutant cysteine of KRAS G12C, while Kobe2602 interferes with binding of Ras to Raf. Salirasib, a farnesylcysteine mimetic, disrupts the membrane association of Ras. Rho-family tools include NSC 23766 and EHT 1864, which inhibit Rac, and CASIN, which targets Cdc42.
Synonyms: K-Ras inhibitor
6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C).
Synonyms: 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).
Synonyms: MRTX 849
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity.
Synonyms: CID-2950007
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines.
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells.
ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRAS-G12C) and could achieve rapid and sustained in vivo target occupancy to induce tumor regression.
BDP9066 is a potent and selective MRCK inhibitor, reducing substrate phosphorylation.
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.
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.
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
Antineoplaston A 10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
Synonyms: 3144; pan-RAS inhibitor-3144
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.
MRTX1257 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, MRTX1257 inhibited KRAS dependent ERKphosphorylation in the H358cell assay with an IC50= 900 pM.
BAY-293 is a potent, cell-active SOS1 inhibitor that disrupts the KRAS-SOS1 interaction with IC50 of 21 nM.
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 17 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 82, has an IC50 of 5 nM.
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 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM.
PHT-7.3 is a selective inhibitor of connector enhancer of kinase suppressor of Ras 1 (Cnk1) pleckstrin homology (PH) domain, which inhibits mut-KRas, but not wild-type KRas cancer cell and tumor growth and signaling.
Synonyms: AMG 510
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.
KRAS G12C inhibitor 5 is a KRas G12C inhibitor extracted from patent WO2017201161A1, Compound example 147.
Synonyms: AMG 510
AMG-510 is a potent, orally bioavailable, and selective KRAS G12C covalent inhibitor with anti-tumor activity.