Ras

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Ras Signaling Pathway Map

Ras Signaling Pathways

Ras Products

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  • Ras Inhibitors (28)
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  • New Ras Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0135New CID-1067700

CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt.

E1051New MRTX1133

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.

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.
S0323 Antineoplaston A10 Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
S1314 Zoledronic acid (ZOL 446) Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
PLoS Pathog, 2022, 18(2):e1010299
J Bone Miner Res, 2022, 10.1002/jbmr.4507
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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.
J Neurosci, 2022, JN-RM-0449-21
Front Microbiol, 2021, 12:628283
Mol Cell, 2020, 80(1):164-174.e4
S5244 Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho.
J Bone Miner Res, 2022, 10.1002/jbmr.4507
Oncol Lett, 2022, 23(2):51
Biomater Sci, 2021, 10.1039/d0bm02107e
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.
S6527 Kobe2602 Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).
S6905 MCP110 MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors.
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
Cell Death Differ, 2019, 26(11):2400-2415
Nat Commun, 2018, 9(1):672
S7330 6H05 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
S7331 K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
Oncotarget, 2016, 7(9):10064-72
S7332 K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
S7333 K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).
S7607 BQU57 BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
PLoS One, 2019, 14(4):e0214764
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Exp Clin Cancer Res, 2022, 41(1):43
Cancer Manag Res, 2020, 12:2057-2067
Mol Oncol, 2018, 12(2):224-238
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.
SLAS Discov, 2022, S2472-5552(22)12517-7
ProQuest, 2020, N/A
Mol Ther Oncolytics, 2019, 14:266-278
S8303 Kobe0065 Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Acta Pharm Sin B, 2019, 9(2):294-303
Cell Death Differ, 2019, 10.1038/s41418-019-0416-4
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.
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.
Nat Commun, 2021, 12(1):2656
J Exp Med, 2021, 218(1)e20201414
Cancer Discov, 2021, 11(8):1913-1922
S8826 BAY-293 BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM.
Clin Cancer Res, 2022, clincanres.4291.2021
SLAS Discov, 2022, S2472-5552(22)12517-7
S8830 Sotorasib (AMG510) Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
Cancer Cell, 2022, S1535-6108(21)00662-0
SLAS Discov, 2022, S2472-5552(22)12517-7
J Exp Med, 2021, 218(1)e20201414
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.
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.
SLAS Discov, 2022, S2472-5552(22)12517-7
Cancer Res, 2021, canres.1153.2021
Cancer Discov, 2021, 11(8):1913-1922
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.
SLAS Discov, 2022, S2472-5552(22)12517-7
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.
Mol Clin Oncol, 2021, 15(1):148
Commun Biol, 2021, 4(1):834
S8959 BI-2852 BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.
S6996New 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.
E0135New CID-1067700

CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt.

E1051New MRTX1133

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.

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.
S0323 Antineoplaston A10 Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
S1314 Zoledronic acid (ZOL 446) Zoledronic acid (ZOL 446, ZA, Zoledronate, CGP-4244, GP42446A, Zometa, Zomera, Aclasta, Reclast), a potent osteoclast inhibitor, induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho. Zoledronic acid (ZA) also induces autophagy.
PLoS Pathog, 2022, 18(2):e1010299
J Bone Miner Res, 2022, 10.1002/jbmr.4507
Hum Cell, 2022, 10.1007/s13577-022-00671-y
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.
J Neurosci, 2022, JN-RM-0449-21
Front Microbiol, 2021, 12:628283
Mol Cell, 2020, 80(1):164-174.e4
S5244 Zoledronic acid monohydrate Zoledronic acid (Zoledronate, CGP-4244) monohydrate, a nitrogen-containing bisphosphonate, is a potent osteoclast inhibitor which induces apoptosis in osteoclasts by inhibiting enzymes of the mevalonate pathway and preventing the isoprenylation of small GTP-binding proteins such as Ras and Rho.
J Bone Miner Res, 2022, 10.1002/jbmr.4507
Oncol Lett, 2022, 23(2):51
Biomater Sci, 2021, 10.1039/d0bm02107e
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.
S6527 Kobe2602 Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).
S6905 MCP110 MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 disrupts the interaction of activated Ras with Raf and is potential for the treatment of human tumors.
S7224 Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.
Acta Pharmacol Sin, 2019, 10.1038/s41401-019-0268-y
Cell Death Differ, 2019, 26(11):2400-2415
Nat Commun, 2018, 9(1):672
S7330 6H05 6H05 is a selective, and allosteric inhibitor of oncogenic K-Ras(G12C).
S7331 K-Ras(G12C) inhibitor 12 K-Ras(G12C) inhibitor 12 is an allosteric inhibitor of oncogenic K-Ras(G12C).
Oncotarget, 2016, 7(9):10064-72
S7332 K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
S7333 K-Ras(G12C) inhibitor 6 K-Ras(G12C) inhibitor 6 is an allosteric, and selective inhibitor of oncogenic K-Ras(G12C).
S7607 BQU57 BQU57, a derivative of RBC8, is a selective GTPase Ral inhibitor relative to the GTPases Ras and RhoA.
PLoS One, 2019, 14(4):e0214764
S7684 Salirasib Salirasib (Farnesylthiosalicylic acid, FTS) is a potent competitive prenylated protein methyltransferase (PPMTase) inhibitor with Ki of 2.6 μM, which inhibits Ras methylation. Salirasib exerts antitumor effects and induces autophagy. Salirasib exerts antitumor effects and induces autophagy. Phase 2.
J Exp Clin Cancer Res, 2022, 41(1):43
Cancer Manag Res, 2020, 12:2057-2067
Mol Oncol, 2018, 12(2):224-238
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.
SLAS Discov, 2022, S2472-5552(22)12517-7
ProQuest, 2020, N/A
Mol Ther Oncolytics, 2019, 14:266-278
S8303 Kobe0065 Kobe0065 is H-Ras-cRaf1 interaction inhibitor, exhibiting potent activity to competitively inhibit the binding of H-Ras·GTP to c-Raf-1 RBD with a Ki value of 46 ± 13 μM.
Acta Pharm Sin B, 2019, 9(2):294-303
Cell Death Differ, 2019, 10.1038/s41418-019-0416-4
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.
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.
Nat Commun, 2021, 12(1):2656
J Exp Med, 2021, 218(1)e20201414
Cancer Discov, 2021, 11(8):1913-1922
S8826 BAY-293 BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM.
Clin Cancer Res, 2022, clincanres.4291.2021
SLAS Discov, 2022, S2472-5552(22)12517-7
S8830 Sotorasib (AMG510) Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.
Cancer Cell, 2022, S1535-6108(21)00662-0
SLAS Discov, 2022, S2472-5552(22)12517-7
J Exp Med, 2021, 218(1)e20201414
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.
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.
SLAS Discov, 2022, S2472-5552(22)12517-7
Cancer Res, 2021, canres.1153.2021
Cancer Discov, 2021, 11(8):1913-1922
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.
SLAS Discov, 2022, S2472-5552(22)12517-7
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.
Mol Clin Oncol, 2021, 15(1):148
Commun Biol, 2021, 4(1):834
S8959 BI-2852 BI-2852 is a potent inhibitor of KRAS that binds with nanomolar affinity to a pocket between switch I and II on RAS. BI-2852 blocks all GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in the low micromolar range in KRAS mutant cells.
S0458 KY1220 KY1220 is a small molecule that destabilizes both β-catenin and Ras, via targeting the Wnt/β-catenin pathway with IC50 of 2.1 μM in HEK293 reporter cells.
E0135New CID-1067700

CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt.

E1051New MRTX1133

MRTX1133 is a highly selective inhibitor of mutant KRAS G12D and can reversibly binds to the activated and inactivated KRAS G12D mutants and inhibit their activity. The specificity of MRTX1133 to KRAS G12D is more than 1000 times that of wild-type KRAS.

S6996New 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.