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Z62954982

SKU: orb2900998

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).

Images & Validation

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Z62954982

Key Properties

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CAS Number1090893-12-1
MW415.46
Purity>98% (HPLC)
FormulaC20H21N3O5S
SMILESO=C(NC1=CC=C(C(=C1)S(=O)(=O)N)C)C=2C=CC=C(OCC=3C(=NOC3C)C)C2
TargetRho
SolubilityIn Vitro: DMSO : 14.29 mg/mL (34.40 mM; Ultrasonic )

Bioactivity

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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. 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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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. 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.
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Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Similar Products

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  • Z62954982

    Z62954982 [orb1693153]

    98.28%

    1090893-12-1

    415.46

    C20H21N3O5S

    100 mg, 1 mg, 25 mg, 10 mg, 1 ml x 10 mM (in DMSO), 200 mg, 5 mg, 50 mg
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Gene Symbol
Rho

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Z62954982 (orb2900998)

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1 g
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2 mg
$ 90.00
5 mg
$ 120.00
10 mg
$ 160.00
25 mg
$ 250.00
50 mg
$ 350.00
100 mg
$ 480.00
500 mg
$ 1,060.00
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