A ROCK1 inhibitor
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GSK25

Item No. 39163

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(4-chloro-2-fluorophenyl)-2-(2-chloro-4-pyridinyl)-N-(6-fluoro-1H-indazol-5-yl)-1,4-dihydro-6-methyl-5-pyrimidinecarboxamide
CAS Number
874119-56-9
Molecular Formula
C24H16Cl2F2N6O
Formula Weight
513.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 10 mg/ml
SMILES
O=C(C1=C(C)N=C(C2=CC(Cl)=NC=C2)N[C@@H]1C3=CC=C(C=C3F)Cl)NC4=CC5=C(C=C4F)NN=C5
InChi Code
InChI=1S/C24H16Cl2F2N6O/c1-11-21(24(35)32-19-6-13-10-30-34-18(13)9-17(19)28)22(15-3-2-14(25)8-16(15)27)33-23(31-11)12-4-5-29-20(26)7-12/h2-10,22H,1H3,(H,30,34)(H,31,33)(H,32,35)/t22-/m1/s1
InChi Key
KZYAHEIPPAPADQ-JOCHJYFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $68

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    1 mg

    $127

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    5 mg

    $399

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    10 mg

    $663

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    Product Description

    GSK25 is an inhibitor of Rho-associated kinase 1 (ROCK1; IC50 = 7 nM for the human kinase).1 It is selective for ROCK1 over p90 ribosomal S6 kinase 1 (RSK1) and p70 ribosomal S6 kinase (p70S6K; IC50s = 398 and 1,000 nM, respectively) and is greater than 100-fold selective over a panel of 31 additional kinases. GSK25 induces relaxation in precontracted isolated rat aortic rings (EC50 = 256 nM). In vivo, GSK25 (30 mg/kg) decreases mean arterial blood pressure in spontaneously hypertensive rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sehon, C.A., Wang, G.Z., Viet, A.Q., et al. Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases. J. Med. Chem. 51(21), 6631-6634 (2008).