| S8031 |
NSC 23766 trihydrochloride
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NSC 23766 trihydrochloride 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.
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J Orthop Translat, 2025, 54:152-166
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Microbiol Spectr, 2025, 13(2):e0222124
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Nat Commun, 2024, 15(1):8159
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| S7319 |
EHop-016
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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.
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Microbiol Spectr, 2025, 13(2):e0222124
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Biochem Biophys Res Commun, 2025, 766:151846
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bioRxiv, 2025, 2025.07.31.668026
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| S7719 |
CCG-1423
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CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription.
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FASEB J, 2025, 39(7):e70505
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Cell Rep, 2024, 43(4):113989
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Bioact Mater, 2023, 26:413-424
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| S7686 |
ML141
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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). This compound is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. It also protects neuroblastoma cells from metformin-induced apoptosis.
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Cell Rep, 2025, 44(8):116025
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Cell Mol Life Sci, 2025, 82(1):127
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EMBO Rep, 2025, 26(21):5239-5269
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| S7482 |
EHT 1864 2HCl
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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.
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Cell Mol Life Sci, 2025, 82(1):127
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Cancer Metab, 2025, 13(1):39
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Sci Adv, 2025, 11(31):eads2310
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| S7293 |
ZCL278
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ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM.
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Am J Physiol Cell Physiol, 2025, 10.1152/ajpcell.00987.2024
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Cell Death Dis, 2024, 15(11):867
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Cancer Commun (Lond), 2023, 43(8):909-937
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| S8749 |
MBQ-167
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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.
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iScience, 2024, 27(6):110139
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Nat Genet, 2022, 10.1038/s41588-022-01191-z
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Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8
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| S8469 |
CCG-203971
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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.
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Biomedicines, 2023, 11(9)2351
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J Cell Physiol, 2020, 235(5):4790-4803
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Small GTPases, 2020, 10.1080/21541248
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| S1721 |
Azathioprine
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Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
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Cancer Cell, 2025, 43(4):776-796.e14
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J Extracell Vesicles, 2024, 13(4):e12426
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J Extracell Vesicles, 2024, 13(4):e12426
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| S8988 |
Rhosin hydrochloride
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Rhosin (G04) hydrochloride (HCl) is a potent, specific inhibitor of RhoA subfamily Rho GTPases with Kd of ~ 0.4 uM. Rhosin hydrochloride induces cell apoptosis.
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J Biol Chem, 2023, 299(6):104749
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J Biol Chem, 2023, 299(6):104749
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Carcinogenesis, 2022, bgac014
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