S8031 |
NSC 23766 trihydrochloride
|
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. |
-
Nat Commun, 2024, 15(1):8159
-
Genes Dis, 2024, 11(3):101035
-
iScience, 2024, 27(6):110139
|
|
S1573 |
Fasudil HCl
|
Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker. |
-
J Immunother Cancer, 2024, 12(11)e009805
-
Sci China Life Sci, 2024, 67(8):1549-1562
-
CNS Neurosci Ther, 2024, 30(11):e70098
|
|
S1314 |
Zoledronic acid (Zoledronate)
|
Zoledronic acid (Zoledronate), 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. |
-
Cells, 2024, 13(10)862
-
Cells, 2024, 13(10)862
-
Cancer Immunol Immunother, 2024, 73(4):62
|
|
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. |
-
Microbiol Spectr, 2024, 12(1):e0239123
-
Theranostics, 2023, 13(2):543-559
-
JCI Insight, 2023, 8(9)e163864
|
|
S7719 |
CCG-1423
|
CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription. |
-
Cell Rep, 2024, 43(4):113989
-
Bioact Mater, 2023, 26:413-424
-
Genome Biol, 2023, 24(1):20
|
|
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). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis. |
-
J Nanobiotechnology, 2024, 22(1):357
-
Int J Mol Sci, 2024, 25(21)11479
-
Genes Cancer, 2024, 15:15-27
|
|
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.
|
-
Nat Commun, 2024, 15(1):2989
-
Dev Cell, 2024, S1534-5807(24)00175-8
-
Cell Rep, 2024, 43(8):114528
|
|
S7293 |
ZCL278
|
ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM. |
-
Cancer Commun (Lond), 2023, 43(8):909-937
-
J Exp Clin Cancer Res, 2022, 41(1):230
-
Front Oncol, 2021, 11:656608
|
|
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. |
-
J Immunother Cancer, 2022, 10(12)e005660
-
J Bone Miner Res, 2022, 10.1002/jbmr.4507
-
Oncol Lett, 2022, 23(2):51
|
|
S8749 |
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. |
-
iScience, 2024, 27(6):110139
-
Nat Genet, 2022, 10.1038/s41588-022-01191-z
-
Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8
|
|
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. |
-
Biomedicines, 2023, 11(9)2351
-
J Cell Physiol, 2020, 235(5):4790-4803
-
Small GTPases, 2020, 10.1080/21541248
|
|
S1721 |
Azathioprine
|
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. |
-
J Extracell Vesicles, 2024, 13(4):e12426
-
J Extracell Vesicles, 2024, 13(4):e12426
-
Cell Rep, 2024, 43(8):114528
|
|
S8988 |
Rhosin hydrochloride
|
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. |
-
J Biol Chem, 2023, 299(6):104749
-
J Biol Chem, 2023, 299(6):104749
-
Carcinogenesis, 2022, bgac014
|
|
S6000 |
CID44216842
|
CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor with EC50s of 1.0 μM and 1.2 μM for Cdc42WT and Cdc42Q61L mutant in GTP binding assay, respectively. |
-
J Extracell Vesicles, 2024, 13(4):e12426
-
bioRxiv, 2023, 2023.07.23.550205
|
|
S6875 |
CASIN
|
CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM. |
|
|
S0765 |
MAZ51
|
MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines. |
|
|
E0345 |
CCG-100602
|
CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling that acts by blocking nuclear translocation of MRTF-A with an IC50 of 10 µM. |
|
|
S6673 |
CCG-222740
|
CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression. |
|
|
E4622New |
RP-102124
|
RP-102124 is a first-in-class allosteric inhibitor of multi-Rac with activity against oncogenic Rac1b. RP-102124 is orally bioavailable and exhibits dose-dependent inhibition of tumor growth in xenograft models. It exhibits potent inhibition of phenotypic characteristics of Rac signaling such as cell migration and cytoskeletal rearrangements. |
|
|
E0102 |
I-191
|
I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.
|
|
|
S5996 |
MLS-573151
|
MLS-573151 is a selective cell division cycle 42 (Cdc42) inhibitor with an EC50 of 2 μM, which acts by blocking the binding of GTP to Cdc42. |
|
|
E2400 |
1A-116
|
1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes. |
-
Zool Res, 2024, 45(2):367-380
|
|
E2385 |
SAR407899 hydrochloride
|
SAR407899 hydrochloride is a selective, potent and ATP-competitive Rho kinase (ROCK) inhibitor, with an IC50 of 135 nM for ROCK-2, and Ki values of 36 and 41 nM for human and rat ROCK-2, respectively. |
|
|
S0890 |
MLS000532223
|
MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM. |
|
|
S6752 |
Y16
|
Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). |
|
|
S8031 |
NSC 23766 trihydrochloride
|
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. |
- Nat Commun, 2024, 15(1):8159
- Genes Dis, 2024, 11(3):101035
- iScience, 2024, 27(6):110139
|
|
S1573 |
Fasudil HCl
|
Fasudil HCl, a potent and selective inhibitor of Rho kinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also a calcium channel blocker. |
- J Immunother Cancer, 2024, 12(11)e009805
- Sci China Life Sci, 2024, 67(8):1549-1562
- CNS Neurosci Ther, 2024, 30(11):e70098
|
|
S1314 |
Zoledronic acid (Zoledronate)
|
Zoledronic acid (Zoledronate), 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. |
- Cells, 2024, 13(10)862
- Cells, 2024, 13(10)862
- Cancer Immunol Immunother, 2024, 73(4):62
|
|
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. |
- Microbiol Spectr, 2024, 12(1):e0239123
- Theranostics, 2023, 13(2):543-559
- JCI Insight, 2023, 8(9)e163864
|
|
S7719 |
CCG-1423
|
CCG-1423 is a specific RhoA pathway inhibitor, which inhibits SRF-mediated transcription. |
- Cell Rep, 2024, 43(4):113989
- Bioact Mater, 2023, 26:413-424
- Genome Biol, 2023, 24(1):20
|
|
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). ML141 is associated with an increase in p38 activation and may induce p38-dependent apoptosis/senescence. ML141 also protects neuroblastoma cells from metformin-induced apoptosis. |
- J Nanobiotechnology, 2024, 22(1):357
- Int J Mol Sci, 2024, 25(21)11479
- Genes Cancer, 2024, 15:15-27
|
|
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.
|
- Nat Commun, 2024, 15(1):2989
- Dev Cell, 2024, S1534-5807(24)00175-8
- Cell Rep, 2024, 43(8):114528
|
|
S7293 |
ZCL278
|
ZCL278 is a selective Cdc42 GTPase inhibitor with Kd of 11.4 μM. |
- Cancer Commun (Lond), 2023, 43(8):909-937
- J Exp Clin Cancer Res, 2022, 41(1):230
- Front Oncol, 2021, 11:656608
|
|
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. |
- J Immunother Cancer, 2022, 10(12)e005660
- J Bone Miner Res, 2022, 10.1002/jbmr.4507
- Oncol Lett, 2022, 23(2):51
|
|
S8749 |
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. |
- iScience, 2024, 27(6):110139
- Nat Genet, 2022, 10.1038/s41588-022-01191-z
- Osteoarthritis Cartilage, 2022, S1063-4584(22)00035-8
|
|
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. |
- Biomedicines, 2023, 11(9)2351
- J Cell Physiol, 2020, 235(5):4790-4803
- Small GTPases, 2020, 10.1080/21541248
|
|
S1721 |
Azathioprine
|
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. |
- J Extracell Vesicles, 2024, 13(4):e12426
- J Extracell Vesicles, 2024, 13(4):e12426
- Cell Rep, 2024, 43(8):114528
|
|
S8988 |
Rhosin hydrochloride
|
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. |
- J Biol Chem, 2023, 299(6):104749
- J Biol Chem, 2023, 299(6):104749
- Carcinogenesis, 2022, bgac014
|
|
S6000 |
CID44216842
|
CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor with EC50s of 1.0 μM and 1.2 μM for Cdc42WT and Cdc42Q61L mutant in GTP binding assay, respectively. |
- J Extracell Vesicles, 2024, 13(4):e12426
- bioRxiv, 2023, 2023.07.23.550205
|
|
S6875 |
CASIN
|
CASIN (Pirl1-related Compound 2) directly inhibits activation of Cdc42/RhoGDI with IC50 of 2 μM. |
|
|
E0345 |
CCG-100602
|
CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling that acts by blocking nuclear translocation of MRTF-A with an IC50 of 10 µM. |
|
|
S6673 |
CCG-222740
|
CCG-222740 is a Rho/MRTF pathway inhibitor. CCG-222740 decreases the activation of stellate cells in vitro and in vivo, by reducing the levels of alpha smooth muscle actin(α-SMA) expression. |
|
|
E4622New |
RP-102124
|
RP-102124 is a first-in-class allosteric inhibitor of multi-Rac with activity against oncogenic Rac1b. RP-102124 is orally bioavailable and exhibits dose-dependent inhibition of tumor growth in xenograft models. It exhibits potent inhibition of phenotypic characteristics of Rac signaling such as cell migration and cytoskeletal rearrangements. |
|
|
E0102 |
I-191
|
I-191 is a potent PAR2 antagonist that inhibits multiple PAR2-induced signaling pathways and functional responses. I-191 also inhibits ERK1/2 phosphorylation, RhoA activation, and inhibition of forskolin-stimulated cAMP accumulation induced by micromolar concentrations of biased ligand GB88.
|
|
|
S5996 |
MLS-573151
|
MLS-573151 is a selective cell division cycle 42 (Cdc42) inhibitor with an EC50 of 2 μM, which acts by blocking the binding of GTP to Cdc42. |
|
|
E2400 |
1A-116
|
1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer, prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes. |
- Zool Res, 2024, 45(2):367-380
|
|
E2385 |
SAR407899 hydrochloride
|
SAR407899 hydrochloride is a selective, potent and ATP-competitive Rho kinase (ROCK) inhibitor, with an IC50 of 135 nM for ROCK-2, and Ki values of 36 and 41 nM for human and rat ROCK-2, respectively. |
|
|
S0890 |
MLS000532223
|
MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases with EC50 ranging from 16 μM to 120 μM. |
|
|
S6752 |
Y16
|
Y16 is an inhibitor of G-protein-coupled Rho GEFs. It blocks the binding of LARG, a DBL-family Rho guanine nucleotide exchange factor, with Rho (Kd = 80 nM). |
|
|