JNK Inhibitor VIII (TCS JNK 6o) is an inhibitor of c-Jun N-terminal kinases with IC50 of 45 nM and 160 nM for JNK-1 and JNK-2, respectively. JNK Inhibitor VIII (TCS JNK 6o) inihibits JNK-1, JNK-2, and JNK-3 with Ki of 2 nM, 4 nM and 52 nM, respectively.
CAS Number: 894804-07-0
Molecular Weight: 356.38
TCS JNK 6o
Chemical Name: N-(4-Amino-5-cyano-6-ethoxy-2-pyridinyl)-2,5-dimethoxybenzeneacetamide
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO 71 mg/mL (199.23 mM)
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: ≥360 days 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
TCS-JNK-6a binds competitively and reversibly to the ATP site. This compound demonstrates a remarkable selectivity profile. Additionally, it shows some inhibition of c-Jun phosphorylation in hepG2 cells. TCS-JNK-6o is a 2, 5-dimethoxy analogue of TCS-JNK-6a with the dimethoxy substitution of the phenyl ring. TCS-JNK-6o shows further gains in potency.
Pharmacokinetic profiles are determined for JNK Inhibitor VIII (TCS-JNK-6o) in Sprague-Dawley rats. JNK Inhibitor VIII (TCS-JNK-6o) showes a short half-life of roughly 1 h, with rapid clearance and barely measurable bioavailability. Microsomal incubation studies revealed that oxidative metabolism is very rapid with this compound.
- Bruce G Szczepankiewicz, et al. J Med Chem. 2006 Jun 15;49
Products are for research use only. Not for human use.
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