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Rhosin hydrochloride is a rho GTPase inhibitor (Kd = 354 nM). Inhibits binding of RhoA to guanine nucleotide exchange factors (GEFs) including LARG, DBL, LBC, p115 RhoGEF and PDZ RhoGEF. Has no effect on the binding of Rac1 or Cdc42 to their respective GEFs. Suppresses RhoA/C-mediated breast cancer cell migration and invasion in vitro. Also induces neurite outgrowth in synergy with NGF.
| Molecular Weight | 394.86 |
| Formula | C20H18N6O.HCl |
| CAS Number | 1281870-42-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL Water 17 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ras Products |
|---|
| AMG410
AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. |
| HRS-4642
HRS-4642 is a selective KRAS(G12D) inhibitor, with Kd value of 0.083 nM. HRS-4642 has anti-cancer activity. HRS-4642 exhibits significant in vivo potency. |
| AZD0022
AZD0022 is a selective and orally active KRASG12D inhibitor. |
| HH0043
HH0043 is an orally active and potent SOS1 inhibitor, with IC50 value of 5.8 nM. |
| BI-2493
BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. |
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