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  3. Z62954982

Z62954982 (Synonyms: ZINC08010136)

Cat. No.: HY-115376
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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).

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Z62954982 Chemical Structure

Z62954982 Chemical Structure

CAS No. : 1090893-12-1

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Description

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)[1][2].

In Vitro

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[1].
Z62954982 (25 μM; 4 hours) significantly reduces the ratio Rac1-GTP/Rac1 and has the most potent inhibitory action (86.0%) in cultured SMCs[1].
Z62954982 (10-100 μM; 72 hours) causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC monolayers[2].

In Vivo

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[3].

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[3]
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.
Molecular Weight

415.46

Formula

C₂₀H₂₁N₃O₅S

CAS No.

1090893-12-1

SMILES

O=C(NC1=CC=C(C)C(S(=O)(N)=O)=C1)C2=CC=CC(OCC3=C(C)ON=C3C)=C2

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Z62954982ZINC08010136Z 62954982Z-62954982ZINC 08010136ZINC-08010136RasPDGF-BBaorticSMCbaselineendothelialbarrierintegrityRac1/Tiam1Inhibitorinhibitorinhibit

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Z62954982
Cat. No.:
HY-115376
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