CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.

Product information

CAS Number: 1085822-09-8

Molecular Weight: 534.82

Formula: C11H9Br4N3O2

Chemical Name: 2-[4, 5, 6, 7-tetrabromo-2-(dimethylamino)-1H-1, 3-benzodiazol-1-yl]acetic acid

Smiles: CN(C)C1=NC2=C(C(Br)=C(Br)C(Br)=C2Br)N1CC(O)=O

InChiKey: PHAOTASRLQMKBE-UHFFFAOYSA-N

InChi: InChI=1S/C11H9Br4N3O2/c1-17(2)11-16-9-7(14)5(12)6(13)8(15)10(9)18(11)3-4(19)20/h3H2,1-2H3,(H,19,20)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 16.67 mg/mL (31.17 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

CK2/ERK8-IN-1 (Compound K66; 0-50 µM; 24 hours; Jurkat cells) treatment displays cytotoxic activity in Jurkat cells.

References:

1. Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65.

Products are for research use only. Not for human use.