Ras

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Ras Products

Catalog No. Information Product Use Citations Product Validations
S1314

Zoledronic Acid

Zoledronic acid (ZA, Zoledronate, CGP-4244), 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.

S2797

Lonafarnib

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.

S7332

K-Ras(G12C) inhibitor 9

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

S7684

Salirasib

Salirasib 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.

S8830

Sotorasib (AMG510)

Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.

S6905New

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.

S8916New

BI-3406

BI-3406 is a potent, orally active and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling with anticancer activities.

S8959New

BI-2852

BI-2852 is a potent KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

S0780New

Oncrasin-1

Oncrasin-1 is a potent and effective inhibitor with anticancer activity. Oncrasin-1 kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 drives abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.

S0023New

K-Ras-IN-1

K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.

S8955New

Sotorasib (AMG510) racemate

Sotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.

S8884New

MRTX849

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.

S7224

Deltarasin

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

S8826

BAY-293

BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM.

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).

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.

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.

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.

S6527

Kobe2602

Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).

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.

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.

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.

S0458New

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
S1314

Zoledronic Acid

Zoledronic acid (ZA, Zoledronate, CGP-4244), 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.

S2797

Lonafarnib

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.

S7332

K-Ras(G12C) inhibitor 9

K-Ras(G12C) inhibitor 9 is an allosteric inhibitor of oncogenic K-Ras(G12C).

S7684

Salirasib

Salirasib 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.

S8830

Sotorasib (AMG510)

Sotorasib (AMG510) is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.This AMG510 is a chiral compound.

S6905New

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.

S8916New

BI-3406

BI-3406 is a potent, orally active and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 6 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling with anticancer activities.

S8959New

BI-2852

BI-2852 is a potent KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based drug design with nanomolar affinity. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.

S0780New

Oncrasin-1

Oncrasin-1 is a potent and effective inhibitor with anticancer activity. Oncrasin-1 kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations. Oncrasin-1 drives abnormal aggregation of PKCι in nucleus of sensitive cells but not in resistant cells.

S0023New

K-Ras-IN-1

K-Ras-IN-1 inhibits K-Ras by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.

S8955New

Sotorasib (AMG510) racemate

Sotorasib (AMG510) racemate is a racemic of AMG-510 which is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.

S8884New

MRTX849

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.

S7224

Deltarasin

Deltarasin is a small molecular inhibitor of KRAS-PDEδ interaction with Kd of 38 nM for binding to purified PDEδ.

S8826

BAY-293

BAY-293 selectively inhibits the KRAS-SOS1 interaction with an IC50 of 21 nM.

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).

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.

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.

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.

S6527

Kobe2602

Kobe2602 is a selective Ras inhibitor that blocks H-Ras GTP binding to c-Raf-1 (Ki = 149 µM).

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.

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.

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.

Catalog No. Information Product Use Citations Product Validations
S0458New

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.