Epiblastin A
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MedKoo CAT#: 561424

CAS#: 16470-02-3

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).


Chemical Structure

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Epiblastin A
CAS# 16470-02-3

Theoretical Analysis

MedKoo Cat#: 561424
Name: Epiblastin A
CAS#: 16470-02-3
Chemical Formula: C12H10ClN7
Exact Mass: 287.0686
Molecular Weight: 287.71
Elemental Analysis: C, 50.10; H, 3.50; Cl, 12.32; N, 34.08

Price and Availability

Size Price Availability Quantity
50.0mg USD 450.0 2 Weeks
100.0mg USD 750.0 2 Weeks
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Synonym: Epiblastin A; AUE;

IUPAC/Chemical Name: 6-(3-Chloro-phenyl)-pteridine-2,4,7-triamine

InChi Key: ZWNKKZSRANLVEW-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: NC1=NC(N)=C2N=C(C3=CC=CC(Cl)=C3)C(N)=NC2=N1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Product Data:

Biological target: CK1 inhibitor; converts epiblast stem cells to ESCs and promotes ESC self-renewal.
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/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 5.75 19.99

Preparing Stock Solutions

The following data is based on the product molecular weight 287.71 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Ursu A, Illich DJ, Takemoto Y, Porfetye AT, Zhang M, Brockmeyer A, Janning P, Watanabe N, Osada H, Vetter IR, Ziegler S, Schöler HR, Waldmann H. Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1. Cell Chem Biol. 2016 Apr 21;23(4):494-507. doi: 10.1016/j.chembiol.2016.02.015. Epub 2016 Mar 31. PMID: 27049670.
In vitro protocol: 1. Ursu A, Illich DJ, Takemoto Y, Porfetye AT, Zhang M, Brockmeyer A, Janning P, Watanabe N, Osada H, Vetter IR, Ziegler S, Schöler HR, Waldmann H. Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1. Cell Chem Biol. 2016 Apr 21;23(4):494-507. doi: 10.1016/j.chembiol.2016.02.015. Epub 2016 Mar 31. PMID: 27049670.
In vivo protocol: TBD

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1: Ursu A, Illich DJ, Takemoto Y, Porfetye AT, Zhang M, Brockmeyer A, Janning P, Watanabe N, Osada H, Vetter IR, Ziegler S, Schöler HR, Waldmann H. Epiblastin A Induces Reprogramming of Epiblast Stem Cells Into Embryonic Stem Cells by Inhibition of Casein Kinase 1. Cell Chem Biol. 2016 Apr 21;23(4):494-507. doi: 10.1016/j.chembiol.2016.02.015. Epub 2016 Mar 31. PubMed PMID: 27049670.