Rho

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Rho Products

New Rho Products
Catalog No. Information Product Use Citations Product Validations
S1314

Zoledronic Acid

Zoledronic acid (ZA), 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.

S8031

NSC 23766

NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.

S7319

EHop-016

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, equally potent inhibition for Rac3.

S1721

Azathioprine

Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.

S7293

ZCL278

ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM.

S6527New

Kobe2602

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

S8826New

BAY-293

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

S8830New

AMG510

AMG-510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.

S8749New

MBQ-167

MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells.

S8707New

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.

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. Phase 2.

S7719

CCG-1423

CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.

S8469

CCG-203971

CCG-203971 is a novel small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription.

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.

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.

S7482

EHT 1864 2HCl

EHT 1864 2HCl is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively.

S7686

ML141

ML141 (CID-2950007), is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7).

S5244

Zoledronic acid monohydrate

Zoledronic acid, 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
S1314

Zoledronic Acid

Zoledronic acid (ZA), 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.

S8031

NSC 23766

NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.

S7319

EHop-016

EHop-016 is a specific Rac GTPase inhibitor with IC50 of 1.1 μM for Rac1 in MDA-MB-435 and MDA-MB-231 cells, equally potent inhibition for Rac3.

S1721

Azathioprine

Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.

S7293

ZCL278

ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM.

S6527New

Kobe2602

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

S8826New

BAY-293

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

S8830New

AMG510

AMG-510 is a potent KRAS G12C covalent inhibitor with potential antineoplastic activity.

S8749New

MBQ-167

MBQ-167 is a potent and dual inhibitor of Rac and Cdc42 with IC50s of 103 nM and 78 nM respectively, in metastatic breast cancer cells.

S8707New

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.

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. Phase 2.

S7719

CCG-1423

CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.

S8469

CCG-203971

CCG-203971 is a novel small-molecule inhibitor of the Rho/MRTF/SRF pathway with the IC50 value of 0.64 μM for SRE.L. It inhibits Rho-mediated gene transcription.

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.

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.

S7482

EHT 1864 2HCl

EHT 1864 2HCl is a potent Rac family GTPase inhibitor with Kd of 40 nM, 50 nM, 60 nM and 250 nM for Rac1, Rac1b, Rac2 and Rac3, respectively.

S7686

ML141

ML141 (CID-2950007), is demonstrated to be a potent, selective and reversible non-competitive inhibitor of Cdc42 GTPase suitable for in vitro assays, with IC50 of 200 nM and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7).

S5244

Zoledronic acid monohydrate

Zoledronic acid, 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.