CAY10746
Code | Size | Price |
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TAR-T36196-1mg | 1mg | £213.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Quantity:
TAR-T36196-5mg | 5mg | £436.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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Quantity:
TAR-T36196-1mL | 1 mL * 10 mM (in DMSO) | £438.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T36196-10mg | 10mg | £610.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T36196-25mg | 25mg | £922.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T36196-50mg | 50mg | £1,219.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T36196-100mg | 100mg | £1,613.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
TAR-T36196-500mg | 500mg | £3,163.00 | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here. |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃
Images
Documents
Further Information
Bioactivity:
CAY10746 is an inhibitor of Rho-associated kinase I (ROCK-I) and ROCK-II (IC50s = 14 and 3 nM, respectively).1It is selective for ROCK-I and ROCK-II 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 anin vitromodel of diabetic retinopathy. It also promotes high glucose-induced vessel regression in mouse retinal explants.
CAS:
2247240-76-0
Formula:
C26H23N3O5
Molecular Weight:
457.5
Pathway:
Cell Cycle/Checkpoint|Stem Cells|Cytoskeletal Signaling
Purity:
0.98
SMILES:
CN(C)C1=CC=C(C(NC2=CC=CC(NC(COC3=CC(OC=CC4=O)=C4C=C3)=O)=C2)=O)C=C1
Target:
ROCK
References
Zhao L, 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. 2019 Dec 12;62(23):10691-10710.