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
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
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/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
5.8 |
19.99 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
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.
| 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.
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.
2: Ren F, Zhu J, Li K, Cheng Y, Zhu X. CK1α-targeting inhibits primary and metastatic colorectal cancer in vitro, ex vivo, in cell-line- derived and patient-derived tumor xenograft mice models. Transl Cancer Res. 2020 Mar;9(3):1903-1913. doi: 10.21037/tcr.2020.02.13. PMID: 35117537; PMCID: PMC8798578.
