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Epiblastin A

Chemical Structure : Epiblastin A

CAS No.: 16470-02-3

Epiblastin A (Casein kinase 1 inhibitor)

Catalog No.: PC-38526Not For Human Use, Lab Use Only.

Epiblastin A is a small molecule ATP-competitive casein kinases 1 (CK1) inhibitor with IC50 values of 0.8, 3.7 and 3.8 uM for CK1δ, CK1ε and CK1α, engages CK1 isoenzymes in cell lysate and induces efficient conversion of mouse epiblast stem cells (EpiSCs) to embryonic stem cells (cESCs).

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Biological Activity

Epiblastin A is a small molecule ATP-competitive casein kinase 1 (CK1) inhibitor with IC50 values of 0.8, 3.7 and 3.8 uM for CK1δ, CK1ε and CK1α, engages CK1 isoenzymes in cell lysate and induces efficient conversion of mouse epiblast stem cells (EpiSCs) to embryonic stem cells (cESCs).
Epiblastin A elicits significant dose-dependent inhibition of the viability of HT29, HCT116, and DLD1 cells with a 48 h IC50 of 6.8, 5.0, and 3.2 μM, respectively.
Epiblastin A attenuated expression of CK1α in CRC primary cultures and PDX samples.
Epiblastin A suppressed tumor volume and tumor weight in a CK1α-dependent manner in DLD1-derived tumor xenograft mice.

Physicochemical Properties

M.Wt 287.71
Formula C12H10CIN7
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(3-Chlorophenyl)-2,4,7-pteridinetriamine

References

1. Ursu A, et al. Cell Chem Biol. 2016 Apr 21;23(4):494-507.

2. Ren F, et al. Transl Cancer Res. 2020 Mar;9(3):1903-1913.

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