| S8955 |
Sotorasib (AMG510) racemate |
Sotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity. |
Selective |
|
| S8884 |
Adagrasib (MRTX849) |
Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling. |
Selective |
|
| S6996 |
LC-2 |
LC-2 is a first PROTAC capable of degrading endogenous KRASG12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRASG12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRASG12C degradation leading to suppression of MAPK signaling.
|
Selective |
|
| S0023 |
K-Ras-IN-1 |
K-Ras-IN-1 (MDK-3017) inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure. |
Selective |
|
| S8499 |
KRpep-2d |
KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
|
Selective |
K-Ras(G12D), IC50: 1.6 nM |
| S8916 |
BI-3406 |
BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities. |
Selective |
K-ras, IC50: 5 nM |
| S8826 |
BAY-293 |
BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM. |
Selective |
K-ras, IC50: 21 nM |
| S8156 |
ARS-853 (ARS853) |
ARS-853 is a selective, covalent KRAS(G12C) inhibitor that inhibits mutant KRAS-driven signaling by binding to the GDP-bound oncoprotein and preventing activation. ARS-853 also induces apoptosis. |
Selective |
K-Ras(G12C), IC50: 2.5 μM |
| S7331 |
K-Ras(G12C) inhibitor 12 |
K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
|
Selective |
|
| S8831 |
MRTX-1257 |
MRTX-1257 is a potent, selective, irreversible, covalent and orally active inhibitor of KRAS G12C with IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. |
Selective |
|
| S7333 |
K-Ras(G12C) inhibitor 6 |
K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C). |
Selective |
|
| S5279 |
Fendiline hydrochloride |
Fendiline hydrochloride is the hydrochloride salt form of Fendiline, which is an L-type calcium channel blocker and also a specific inhibitor of K-Ras plasma membrane targeting with no detectable effect on the localization of H- and N-Ras. |
Selective |
|
| S8830 |
Sotorasib (AMG510) |
Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound. |
Selective |
|
| S7330 |
6H05 |
6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
|
Selective |
|
| S7224 |
Deltarasin |
Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
|
Selective |
|
| S8707 |
ARS-1620 |
ARS-1620 is a potent, orally bioavailable covalent inhibitor of KRASG12C and could achieve rapid and sustained in vivo target occupancy to induce tumor regression. |
Selective |
|
| S7332 |
K-Ras(G12C) inhibitor 9 |
K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
|
Selective |
|
| S2797 |
Lonafarnib (SCH66336) |
Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3. |
Pan |
K-ras-4B, IC50: 5.2 nM |
