894804-07-0 Usage
Description
TCS JNK 6o, also known as JNK Inhibitor VIII, is an aminopyridine compound that belongs to the c-Jun amino terminal kinases (JNKs) family of MAP kinases. It is a potent inhibitor of JNK1, JNK2, and JNK3 with Ki values of 2, 4, and 52 nM, respectively. TCS JNK 6o has been shown to suppress apoptosis, caspase cleavage, and cytochrome C release, making it a promising candidate for various applications in different industries.
Uses
Used in Pharmaceutical Industry:
TCS JNK 6o is used as a JNK inhibitor for the treatment of neurodegeneration, rheumatoid arthritis, inflammation, cancer, and diabetes. Its ability to inhibit the phosphorylation of the JNK substrate c-Jun in HepG2 cells (EC50 = 920 nM) without affecting the expression of IL-6, IL-8, or COX-2 makes it a valuable tool in drug discovery and development.
Used in Research Applications:
TCS JNK 6o is used as a research tool for studying the role of JNKs in various cellular processes and diseases. Its high specificity and potency in inhibiting JNK1, JNK2, and JNK3 make it an ideal compound for investigating the molecular mechanisms underlying the activation and regulation of JNKs in different stress conditions and diseases.
Used in Drug Discovery:
TCS JNK 6o is used in drug discovery as a lead compound for the development of novel therapeutic agents targeting JNKs. Its ability to inhibit JNKs with high potency and selectivity makes it a promising starting point for the design and synthesis of new drugs with improved pharmacological properties and therapeutic efficacy.
in vitro
cs jnk 6o, in a dose-dependent manner, inhibits phosphorylation of c-jun (ec50 = 920 nm) and prevents collagen-induced platelet aggregation. at low collagen concentrations (0.2 and 0.5 μg/ml), platelet aggregation was totally or partially impaired by 10 μm cs jnk 6o, whereas at a high collagen concentration (5 μg/ml), tcs jnk 6o had no effect [2].
in vivo
. pharmacokinetic profiles were studied for tcs jnk 6o in sprague-dawley rats. tcs jnk 6o showed a short half-life of about 1 hour, with barely measurable bioavailability and rapid clearance. microsomal incubation studies revealed that the oxidative metabolism of tcs jnk 6o was very rapid [1]
IC 50
45 nm for jnk1 and 160 nm for jnk2 [1]
references
[1] szczepankiewicz bg1, kosogof c, nelson lt, liu g, liu b, zhao h, serby md, xin z, liu m, gum rj, haasch dl, wang s, clampit je, johnson ef, lubben th, stashko ma, olejniczak et, sun c, dorwin sa, haskins k, abad-zapatero c, fry eh, hutchins cw, sham hl, rondinone cm, trevillyan jm. aminopyridine-based c-jun n-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity. j med chem. 2006 jun 15;49(12):3563-80.[2] kauskot a, adam f, mazharian a, ajzenberg n, berrou e, bonnefoy a, rosa jp, hoylaerts mf, bryckaert m. involvement of the mitogen-activated protein kinase c-jun nh2-terminal kinase 1 in thrombus formation. j biol chem. 2007 nov 2;282(44):31990-9.
Check Digit Verification of cas no
The CAS Registry Mumber 894804-07-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,9,4,8,0 and 4 respectively; the second part has 2 digits, 0 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 894804-07:
(8*8)+(7*9)+(6*4)+(5*8)+(4*0)+(3*4)+(2*0)+(1*7)=210
210 % 10 = 0
So 894804-07-0 is a valid CAS Registry Number.
894804-07-0Relevant articles and documents
Inhibitors of c-Jun N-terminal kinases
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Page/Page column 44, (2008/06/13)
The present invention relates to compounds that are inhibitors of c-jun N-terminal kinase 1, 2, or 3 (JNK1, JNK2, or JNK3), compositions containing the compounds and the use of the compounds in the prevention or treatment of disorders regulated by the activation of JNK1, JNK2 and JNK3.
