Ras

Inhibitory Selectivity

Isoform-specific Inhibitors

Ras Products

All (28) Ras Inhibitors (26) Ras Chemicals (2) New Ras Products

Catalog No.	Information	Product Use Citations	Product Validations
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
E1051^New	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.
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 Eur J Cancer, 2022, 170:91-102 SLAS Discov, 2022, 27(2):107-113
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.
E1157^New	Pan-RAS-IN-1 Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRas^G12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.
E1071^New	ASP2453 ASP2453, a potent, selective and covalent KRAS G12C inhibitor, inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 of 40 nM.
E1047^New	NAV-2729 NAV-2729, an inhibitor of Arf6 activation which directly binds to Arf6, also inhibits all Arf guanine nucleotide exchange factors (ArfGEFs) with a strongest effect against BRAG2 and Arf1 .
E0135^New	CID-1067700 CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt.
S7224	Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with K_d 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
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
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.
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).	Biomedicines, 2022, 10(3)592 Oncotarget, 2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
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
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
S8707	ARS-1620 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.	SLAS Discov, 2022, 27(2):107-113 Nat Commun, 2021, 12(1):2656 J Exp Med, 2021, 218(1)e20201414
S6527	Kobe2602 Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).
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.
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.
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, 27(2):107-113 SLAS Discov, 2022, S2472-5552(22)12517-7 Cancer Res Commun, 2022, 2(5):342-352
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.
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
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
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.
S6996^New	LC-2 LC-2 is a first PROTAC capable of degrading endogenous KRAS^G12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRAS^G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS^G12C degradation leading to suppression of MAPK signaling.
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.

Catalog No.	Information	Product Use Citations	Product Validations
S7332	K-Ras(G12C) inhibitor 9 K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).
E1051^New	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.
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 Eur J Cancer, 2022, 170:91-102 SLAS Discov, 2022, 27(2):107-113
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.
E1157^New	Pan-RAS-IN-1 Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRas^G12D-GppNHp with a Kd less than 20 μM in MST, ITC and NMR assays, also binds to Ras proteins and exhibits lethality in cells partially dependent on expression of Ras proteins.
E1071^New	ASP2453 ASP2453, a potent, selective and covalent KRAS G12C inhibitor, inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 of 40 nM.
E1047^New	NAV-2729 NAV-2729, an inhibitor of Arf6 activation which directly binds to Arf6, also inhibits all Arf guanine nucleotide exchange factors (ArfGEFs) with a strongest effect against BRAG2 and Arf1 .
E0135^New	CID-1067700 CID-1067700 (ML282) is a pan-GTPase inhibitor with a ki of 12.89 nM for Rab7wt.
S7224	Deltarasin Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with K_d 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
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
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.
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).	Biomedicines, 2022, 10(3)592 Oncotarget, 2016, 7(9):10064-72	(A) Proliferation of Calu-1 cells after SAHA and K-ras inhibitor (K-ras C12) treatment. Calu-1 cells, containing an activating G12C K-ras mutation, were treated with SAHA (2.5 mM) and K-ras C12 (10 mM) for 24 h and analyzed as in Figure Figure1A.1A. (B) Immunoblotting of Calu-1 cells treated with inhibitors. Cells were treated with inhibitors as indicated for 24 hrs. Cell lysates were collected and immunoblotted with antibodies indicated.
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
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
S8707	ARS-1620 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.	SLAS Discov, 2022, 27(2):107-113 Nat Commun, 2021, 12(1):2656 J Exp Med, 2021, 218(1)e20201414
S6527	Kobe2602 Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).
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.
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.
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, 27(2):107-113 SLAS Discov, 2022, S2472-5552(22)12517-7 Cancer Res Commun, 2022, 2(5):342-352
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.
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
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
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.

Catalog No.	Information	Product Use Citations	Product Validations
S6996^New	LC-2 LC-2 is a first PROTAC capable of degrading endogenous KRAS^G12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRAS^G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS^G12C degradation leading to suppression of MAPK signaling.
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.

Catalog No.

Information

Product Use Citations

Product Validations

S6996^New

LC-2

LC-2 is a first PROTAC capable of degrading endogenous KRAS^G12C with DC50s between 0.25 μM and 0.76 μM. LC-2 covalently binds KRAS^G12C with a MRTX849 warhead and recruits the E3 ligase VHL, inducing rapid and sustained KRAS^G12C degradation leading to suppression of MAPK signaling.

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.

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Ras

Inhibitory Selectivity

Isoform-specific Inhibitors

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