A ROCK1 and ROCK2 inhibitor
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CAY10746

Item No. 29814

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(dimethylamino)-N-[3-[[2-[(4-oxo-4H-1-benzopyran-7-yl)oxy]acetyl]amino]phenyl]-benzamide
CAS Number
2247240-76-0
Molecular Formula
C26H23N3O5
Formula Weight
457.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
239, 247, 305 nm
SMILES
CN(C)C1=CC=C(C(NC2=CC=CC(NC(COC3=CC(OC=CC4=O)=C4C=C3)=O)=C2)=O)C=C1
InChi Code
InChI=1S/C26H23N3O5/c1-29(2)20-8-6-17(7-9-20)26(32)28-19-5-3-4-18(14-19)27-25(31)16-34-21-10-11-22-23(30)12-13-33-24(22)15-21/h3-15H,16H2,1-2H3,(H,27,31)(H,28,32)
InChi Key
WVGDUQVQWLHVEA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    500 µg

    $169

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    1 mg

    $319

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    5 mg

    $753

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    Product Description

    CAY10746 is an inhibitor of Rho-associated kinase I (ROCK1) and ROCK2 (IC50s = 14 and 3 nM, respectively).1 It is selective for ROCK1 and ROCK2 over PKA (IC50 = >10,000 nM) and over 387 recombinant human protein kinases in a panel of 394 kinases (IC50s = >10,000 nM for all) but does inhibit LIM kinase 2 (LIMK2), Aurora A, Aurora B, cGMP-dependent protein kinase 1α (PKG1α), and PKG1β (IC50s = 46, 1,072, 1,239, 517, and 660 nM, respectively). CAY10746 (0.1-10 µM) inhibits phosphorylation of the ROCK target protein MYPT1 in SH-SY5Y cells. It also inhibits migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 1 µM. CAY10746 (1 µM) protects isolated mouse retinal neurons from apoptosis and oxidative stress induced by high glucose in an in vitro model of diabetic retinopathy. It also promotes high glucose-induced vessel regression in mouse retinal explants.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zhao, L., Li, Y., Wang, Y., et al. Discovery of 4H-chromen-4-one derivatives as a new class of selective Rho kinase (ROCK) inhibitors, which showed potent activity in ex vivo diabetic retinopathy models. J. Med. Chem. 62(23), 10691-10710 (2019).