Specification
Description
Epiblastin A is a Casein Kinase 1 (CK1) inhibitor. Epiblastin A engages CK1 isoenzymes in cell lysate and induces efficient conversion of epiblast stem cells (EpiSCs) into embryonic stem cells (cESCs).
Synonyms
Epiblastin A; AUE
IUPAC Name
6-(3-Chloro-phenyl)-pteridine-2,4,7-triamine
Canonical SMILES
NC1=NC(N)=C2N=C(C3=CC=CC(Cl)=C3)C(N)=NC2=N1
InChI
InChI=1S/C12H10ClN7/c13-6-3-1-2-5(4-6)7-9(14)18-11-8(17-7)10(15)19-12(16)20-11/h1-4H,(H6,14,15,16,18,19,20)
InChI Key
ZWNKKZSRANLVEW-UHFFFAOYSA-N
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Storage
Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
Biological Target
CK1 inhibitor; converts epiblast stem cells to ESCs and promotes ESC self-renewal.
Drug Formulation
This drug may be formulated in DMSO
Elemental Analysis
C, 50.10; H, 3.50; Cl, 12.32; N, 34.08
HS Tariff Code
2934.99.9001
In Vitro Activity
Target engagement by Epiblastin A was investigated in human HCT116 colorectal carcinoma cells because all CK1 isoenzymes could be detected in the cell lysate (see Figure S3A). After incubation of the HCT116 cell lysate with increasing concentrations of Epiblastin A (1, 10, and 100 μM, respectively) and addition of the probe, labeled proteins were isolated using streptavidin-coated beads and analyzed by means of immunoblotting. As shown in Figure 5A, in the absence of inhibitor, CK1α/δ/ɛ are labeled by the reagent. Addition of Epiblastin A to the cell lysate in increasing concentrations impairs labeling and, therefore, binding of the ATP probe to the kinase. This result proves engagement of the three CK1α/δ/ɛ isoenzymes by Epiblastin A in HCT116 cell lysate.
Reference: Cell Chem Biol. 2016 Apr 21;23(4):494-507. https://pubmed.ncbi.nlm.nih.gov/27049670/
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Stock Solution Storage
0-4 °C for short term (days to weeks), or -20 °C for long term (months).