pan-KRAS-IN-2 (compound 6) is a pan inhibitor of with IC50s ≤10 nM for KRAS WT and mutants (G12D, G12C, G12V, G12S, G12A, Q61H), and ＞10 μM for KRAS G13D, respectively[1].
SOS1-IN-13 is a potent son of sevenless homolog 1 (SOS1) inhibitor with IC50s of 6.5 nM and 327 nM for SOS1 and pERK, respectively. SOS1-IN-13 can be used for researching anticancer[1].
KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor for potential treatment in cancer.
K-Ras-IN-2 (Compound CHI-000-667) is a K-Ras antagonist, and can be used for tumor research[1].
CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF[1][2].
KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 20)[1].
KRAS G12C inhibitor 31 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 1. KRAS G12C inhibitor 31 can be used for the research of cancer[1].
6H05 is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C). IC50 value:Target: K-Ras G12C6H05 gives the greatest degree of modification, which allosterically modifies the oncogenic G12C mutant of highly homologous protein H-Ras without affecting wild-type K-Ras [1]. 6H05 can be used as an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors [2].
PROTAC KRAS G12C degrader-3 (Comp 283) is a potent KRAS G12C degrader for cancer research[1].
KRAS G12C inhibitor 42 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 42 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2020146613A1, compound 10)[1].
KRAS G12C inhibitor 56 (compound IC-6) is a potent SOS1 inhibitor with an IC50 of 1.6 nM. KRAS G12C inhibitor 56 can be used in cancer research[1].
Y16 is an inhibitor of G-protein–coupled Rho GEFs; works synergistically with Rhosin/G04 in inhibiting LARG-RhoA interaction, RhoA activation, and RhoA-mediated signaling functions.IC50 value: Target: RhoA inhibitorY16 binds to this catalytic fragment of LARG with a Kd of ～76 ± 8 nM. Y16 was able to inhibit the GDP dissociation from RhoA catalyzed by LARG dose dependently without affecting the GEF reactions of Rac1 and Cdc42 catalyzed by TrioN and Intersectin, respectively. The N983A mutant lost the binding ability to Y16 with a Kd > 500 μM, whereas the K979A and E982A mutants showed a reduced affinity with Kd values of 0.47 and 2.1 μM, respectively. At 2.5 μM each, Rhosin and Y16 inhibited ～50% RhoA-GTP content, and at 5 μM each ～80% RhoA-GTP stimulated by serum, which were much more potent than the effect of Rhosin/G04 or Y16 acting alone (～80% inhibition at 30 μM). Even under a higher concentration of Y16 and Rhosin/G04 combination (50 μM each) when endogenous RhoA-GTP content was effectively suppressed, no effect on Rac1-GTP or Cdc42-GTP content in cells was observed. Although Rhosin/G04 or Y16 administration alone caused ～50% inhibition of RhoA activity at 10 μM, combined Rhosin/G04 and Y16 reached 70% inhibition of RhoA-GTP or the downstream p-MLC when each was at 2.5 μM.
AMG-510 racemate is the racemate of AMG-510. AMG-510 is a potent KRAS G12C covalent inhibitor.
JDQ-443 (example 1a) is a covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1)[1].
pan-KRAS-IN-4 (compound 5) is a potent inhibitor of KRAS with IC50s of 0.37 nM (Kras G12C), 0.19 nM (Kras G12V), respectively[1].
KRAS degrader-1 (compound 1) is a potent KRAS degrader. KRAS degrader-1 target specific proteins for degradation through the autophagy-lysosomal degradation pathway[1].
SOS1-IN-16 (Comp 54) is a selective inhibitor of SOS1 with an IC50 of 7.2 nM. SOS1-IN-16 has inhibitory activity of CYP3A4 when using testosterone as a substrate, with an IC50 of 8.9μM. SOS1-IN-16 can be used for cancer research[1].
CX-5011 is a CK2 inhibitor. CX-5011 also induces Rac1 activation. CX-5011 induces apoptosis and induces cancer cell death[1][2].
KRAS G12C inhibitor 21 is a KRAS G12C inhibitor extracted from patent WO2021219090A1, example 7[1].
ML141(CID-2950007) is a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase(IC50=200 nM) with low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). IC50 value: 200 nM [1]Target: Cdc42 inhibitorin vitro: In the primary HTS bead-based assay using 1 mM EDTA and 100 nM BODIPY-FL-GTP, potency for CID2950007 was IC50 = 2.6 and 5.4 μM for Cdc42 wild type and activated mutant, respectively [1]. ML141 exposure also enhanced the ability of TMX to suppress BLBC cell growth, through both induction of cell death and suppression of cell division [2]. in vivo: Treatment with ML141 + TMX caused a suppression of further tumour growth in vivo [2]. Parallel suppression of the conserved brain CDC42 activity by intracerebroventricular ML141 injection caused acute anxiety in mice [3]. using a pilocarpine-induced epileptic model, we found that pretreatment with ML141, a specific inhibitor of Cdc42, reduces seizure severity [4].
KRAS G12C inhibitor 41 is a potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12C inhibitor 41 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021129824A1, compound 121)[1].
GDC-6036-NH is from patent WO2020097537A2, and a precursor of compound 17 a/b. Compound 17 a/b is a RAS inhibitor and can be used in cancer research[1].
NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase, used for cancer treatment.
ML-098 (CID-7345532) is an activator of the GTP-binding protein Rab7 with an EC50 of 77.6 nM.
KRAS G12C inhibitor 43 (compound 59) is a potent KRAS G12C inhibitor. KRAS G12C inhibitor 43 shows antimigration and anti-proliferative activity with IC50s of 0.001-1 µM, >1 µM, >1 µM for H358, A549, HCC cells ,respectively[1].
KRAS G12C inhibitor 15 is a potent KRAS G12C inhibitor extracted from patent WO2019110751A1, compound 22, has an IC50 of 5 nM[1].
RAS-IN-2 (Compound A122) is a potent RAS(ON)MULTI inhibitor and can be used for the research of cancer[1].
ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.
KRAS G12C inhibitor 28 is a KRAS G12C inhibitor with an IC50 of 57 nM. KRAS G12C inhibitor 28 has antitumor effects (WO2021113595A1; Example 1)[1].
Rasarfin is a dual Ras and ARF6 inhibitor[1].