Ras

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1314 Zoledronic acid (ZOL 446) <1 mg/mL 0.004 mg/mL ''<1 mg/mL
S2797 Lonafarnib (SCH66336) <1 mg/mL 127 mg/mL '127 mg/mL
S7332 K-Ras(G12C) inhibitor 9 <1 mg/mL 53 mg/mL <1 mg/mL
E1157 Pan-RAS-IN-1 <1 mg/mL 6 mg/mL 6 mg/mL
E0135 CID-1067700 <1 mg/mL 78 mg/mL '''<1 mg/mL
S8830 Sotorasib (AMG510) <1 mg/mL 100 mg/mL '100 mg/mL
S0023 K-Ras-IN-1 <1 mg/mL 41 mg/mL '41 mg/mL
S7224 Deltarasin <1 mg/mL 100 mg/mL 100 mg/mL
S8826 BAY-293 <1 mg/mL 90 mg/mL 90 mg/mL
S6905 MCP110 <1 mg/mL 100 mg/mL 100 mg/mL
S7330 6H05 100 mg/mL 100 mg/mL 100 mg/mL
S7331 K-Ras(G12C) inhibitor 12 <1 mg/mL 27 mg/mL <1 mg/mL
S8303 Kobe0065 <1 mg/mL 89 mg/mL 13 mg/mL
S7333 K-Ras(G12C) inhibitor 6 <1 mg/mL 81 mg/mL 30 mg/mL
S7607 BQU57 <1 mg/mL 66 mg/mL 20 mg/mL
S8707 ARS-1620 <1 mg/mL 86 mg/mL 60 mg/mL
S6527 Kobe2602 <1 mg/mL 84 mg/mL 40 mg/mL
S8959 BI-2852 <1 mg/mL 100 mg/mL ''''23 mg/mL
S0323 Antineoplaston A10 <1 mg/mL 49 mg/mL '''<1 mg/mL
S5279 Fendiline hydrochloride -1 mg/mL 70 mg/mL -1 mg/mL
S8884 Adagrasib (MRTX849) <1 mg/mL 100 mg/mL '50 mg/mL
S8499 KRpep-2d 100 mg/mL -1 mg/mL -1 mg/mL
S8156 ARS-853 (ARS853) <1 mg/mL 86 mg/mL 1 mg/mL
S8916 BI-3406 <1 mg/mL 92 mg/mL ''92 mg/mL
S8955 Sotorasib (AMG510) racemate <1 mg/mL 100 mg/mL 100 mg/mL
S8831 MRTX-1257 <1 mg/mL 100 mg/mL ''30 mg/mL
S5244 Zoledronic acid monohydrate <1 mg/mL 0.01 mg/mL <1 mg/mL
S6996 LC-2 <1 mg/mL 100 mg/mL ''<1 mg/mL
S0458 KY1220 <1 mg/mL 63 mg/mL <1 mg/mL

亜型選択性的な製品

Ras製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

S7332

K-Ras(G12C) inhibitor 9

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

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. Phase 2.

E1051

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.

E1157

Pan-RAS-IN-1

Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-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

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

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

CID-1067700

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

S8830

Sotorasib (AMG510)

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

S0730

(Rac)-Antineoplaston A10

(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is an inhibitor of Ras that is potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer.

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.

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.

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).

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).

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.

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.

S8884

Adagrasib (MRTX849)

Adagrasib (MRTX849) is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling.

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.

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.

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.

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.

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.

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.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

S7332

K-Ras(G12C) inhibitor 9

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

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. Phase 2.

E1051

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.

E1157

Pan-RAS-IN-1

Pan-RAS-IN-1, a pan-Ras inhibitor, binds to KRasG12D-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

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

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

CID-1067700

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

S8830

Sotorasib (AMG510)

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

S0730

(Rac)-Antineoplaston A10

(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is an inhibitor of Ras that is potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer.

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.

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.

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).

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).

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.

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.

S8884

Adagrasib (MRTX849)

Adagrasib (MRTX849) is a potent, selective, and covalent KRAS G12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRAS G12C and inhibits KRAS-dependent signaling.

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.

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.

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.

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.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

Tags: Ras inhibitor|Ras agonist|Ras activator|Ras inducer|Ras antagonist|Ras signaling pathway|Ras assay kit