The AGC (PKA/PKG/PKC) family of serine-threonine kinases includes ROCK (Rho-associated protein kinase). Animals such as chicken, zebrafish, Xenopus, and mammals also have ROCKs (ROCK1 and ROCK2). With a molecular weight of 158 kDa, human ROCK1 is a significant RhoA small GTPase downstream effector. A kinase domain, an acoiled-coil region, and a Pleckstrin homology (PH) domain make up a mammalian ROCK. If RhoA-GTP is absent, the kinase activity of ROCKs is reduced by an autoinhibitory intramolecular fold. Since ROCK is a downstream effector protein of the small GTPase Rho, one of the primary regulators of the cytoskeleton, ROCK is involved in a variety of different cellular phenomena.
Structure | Cat No. | Product Name | CAS No. | Product Description |
---|---|---|---|---|
V9236 | 1A-116 | 1430208-73-3 | 1A-116 is a Rac1 inhibitor specific for the W56 residue, which can effectively prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. | |
V1571 | 6H05 TFA | 2061344-88-3 | 6H05 TFA (6H-05; 6 H05), the trifluoroacetic acd salt of 6H05, is a potent, covalent, selective and allosteric inhibitor of K-Ras (G12C) which is oncogenic. | |
V1563 | Azathioprine (BW 57-322) | 446-86-6 | Azathioprine (BW-57322; BW 57-322; Imuran; Azasan; Imurel; AZA; AZTP) is an approved immunosuppressive drug (prodrug of 6-MP) used in the treatment of organ transplantation and autoimmune diseases. | |
V17607 | CASIN | 425399-05-9 | CASIN is a novel, potent and selective inhibitor of Cdc42 GTPase, a small GTPase of the Rho-subfamily that plays important roles in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. | |
V17716 | CCG-100602 | 1207113-88-9 | CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. | |
V1567 | CCG-1423 | 285986-88-1 | CCG-1423 (CCG1423;CCG 1423) is a novel, potent and specific small-molecule inhibitor of RhoA signaling pathway with potential antitumor activity. | |
V17719 | CCG-222740 | 1922098-69-8 | CCG-222740 (CCG222740) is a novel and potent Rho/myocardin-related transcription factor (MRTF)/SRF inhibitor. | |
V1562 | EHop-016 | 1380432-32-5 | EHop-016 (EHOP016;EHop 016)is a novel, potent and selective small molecule inhibitor of Rac GTPase with potential antineoplastic activity. | |
V1566 | EHT 1864 2HCl | 754240-09-0 | EHT 1864 2HCl (EHT-1864; EHT1864),the dihydrochloride salt of EHT-1864,is a potent and novel Rac family GTPase inhibitor with important biological activity. | |
V1570 | K-Ras inhibitor 12 | 1469337-95-8 | K-Ras(G12C) inhibitor 12 is a co-valent and allosteric inhibitor of K-Ras G12C with potential antitumor activity. | |
V1572 | K-Ras(G12C) inhibitor 9 | 1469337-91-4 | K-Ras(G12C) inhibitor 9 is a novel, covalent and allosteric inhibitor of K-RAS G12C mutant with potential anticancer activity. | |
V1569 | ML141(CID-2950007) | 71203-35-5 | ML141 (also called CID-2950007; ML-141; CID2950007; ML 141)is a novel potent, selective and reversible non-competitive inhibitor of Rho family GTPase cdc42 with potential anticancer activity. | |
V40875 | MLS-573151 | 10179-57-4 | MLS-573151 is a novel, specific, cell permeable inhibitor of Cdc42 (IC50 = 2 μM). | |
V1561 | NSC 23766 | 733767-34-5 | NSC 23766 (NSC-23766; NSC23766) is a novel, selective and potent inhibitor of Rac GTPase withanti-influenza virus activity. | |
V0012 | NSC-23766 3HCl | 1177865-17-6 | NSC23766 3HCl, the salt form of NSC23766, is a novel and potent inhibitor of Rac GTPase that targets the activation of Rac by guanine nucleotide exchange factors (GEFs) with an IC50 of less than 50 μM in a test conducted without using cells; NSC23766 does not inhibit the closely related targets, Cdc42 or RhoA. | |
V1568 | Salirasib (Farnesyl Thiosalicylic Acid) | 162520-00-5 | Salirasib (known also as S-Farnesylthiosalicylic acid; Farnesyl Thiosalicylic Acid; FTS),a salicylic acid analog, is a potent and competitive prenylated protein methyltransferase (PPMTase) inhibitor with potential antineoplastic activity. | |
V2029 | SAR407899 HCl | 923262-96-8 | SAR407899 HCl is a novel, potent, selective, and ATP-competitive ROCK inhibitor with an IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively. | |
V1564 | ZCL278 | 587841-73-4 | ZCL278 (ZCL-278; ZCL 278) is a potent,cell-permeable and selective Cdc42 GTPase inhibitor with potential anticancer activity. | |
V1560 | Zoledronic Acid (Zoledronate; CGP 42446) | 118072-93-8 | Zoledronic acid (Zoledronate; CGP-42446; CGP42446A; ZOL-446; Zometa; Reclast) is potent bisphosphonate with anti-bone-resorption activity. |