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D4476

Cat. No. M2610
D4476 Structure
Synonym:

Casein Kinase I Inhibitor

Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 100  USD100 In stock
50mg USD 250  USD250 In stock
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Quality Control & Documentation
Biological Activity

D4476 is a selective inhibitor of casein kinase 1 (CK1) and TGF-β type-I receptor (ALK5) with IC50 of 0.3 µM and 0.5 µM, respectively.

Chemical Information
Molecular Weight 398.41
Formula C23H18N4O3
CAS Number 301836-43-1
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Morvarid Siri, et al. Casein Kinase-1-Alpha Inhibitor (D4476) Sensitizes Microsatellite Instable Colorectal Cancer Cells to 5-Fluorouracil via Authophagy Flux Inhibition

[2] Pengfei Shi, et al. CK1 inhibitor affects in vitro maturation and developmental competence of bovine oocytes

[3] Xing Feng, et al. Ubiquitination of UVRAG by SMURF1 promotes autophagosome maturation and inhibits hepatocellular carcinoma growth

[4] Jenny Bain, et al. The selectivity of protein kinase inhibitors: a further update

[5] Graham Rena, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a

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Keywords: D4476, Casein Kinase I Inhibitor supplier, Casein Kinase, inhibitors, activators


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