Z62954982

Research use only, not for human use.

Z62954982 (ZINC08010136) is a selective inhibitor of Rac1, which stunts the growth and branching of neurons.

Z62954982 (ZINC08010136) is a potent, selective and cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982 disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA).

Z62954982 (5-100 μM; 4 hours) reduces the intracellular levels of Rac1- GTP in a concentration-dependent manner,and shows the most potent inhibitory action with an IC50 of 12.2 μM in Human SMCs.Z62954982 (25 μM; 4 hours) significantly reduces the ratio Rac1-GTP/Rac1 and has the most potent inhibitory action (86.0%) in cultured SMCs.Z62954982 (10-100 μM; 72 hours) causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC monolayers.

Z62954982 (intraperitoneal?injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks) has no obvious signs of toxicity and decreases both phosphorylation of p38 as well as secreted IL-6 in PASMCs in response to hypoxia in both abr-/- and?bcr-/- mice.Animal Model:Male?bcr-/-,?abr-/-?and?wt?mice (8 to 10-week-old littermates) are exposed to hypoxia (10% O2) or normoxia (21% O2) for 3 weeks Dosage:10 mg/kg or 20 mg/kg Administration:Intraperitoneal?injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks Result:Promoted phosphorylation of p38 MAPK and increased IL-6 in Hypoxia in mice.

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Cell Cycle/DNA Damage

Rho

Rho

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1090893-12-1

415.46

C20H21N3O5S

>98% (HPLC)

In Vitro:?DMSO : 14.29 mg/mL (34.40 mM; Ultrasonic )

O=C(NC1=CC=C(C(=C1)S(=O)(=O)N)C)C=2C=CC=C(OCC=3C(=NOC3C)C)C2

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(-20℃)

With Ice Pack

≥ 2 years