TCS JNK 5a

Alias: JNK Inhibitor IX; CS JNK 5a; TCS-JNK-5a; SC 202671; SC202671; SC-202671
Cat No.:V0473 Purity: ≥98%
TCS JNK 5a (alsoknown asJNK Inhibitor IX; TCS JNK-5a) is a novel, highly selective and potent JNK (c-Jun N-terminal Kinase) inhibitor with potential antineoplastic activity.
TCS JNK 5a Chemical Structure CAS No.: 312917-14-9
Product category: JNK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

TCS JNK 5a (also known as JNK Inhibitor IX; TCS JNK-5a) is a novel, highly selective and potent JNK (c-Jun N-terminal Kinase) inhibitor that may have anti-cancer effects. With pIC50 values of 6.5 and 6.7, it inhibits JNK2/3. With pIC50 values of < 5.0, it has no or minimal effects on EGFR, ErbB2, VegFr2, Src, Tie-2, Alk5, c-Fms, CDK-2, GSK3β and PLK1. Human Jurkat T cells were exposed to the JNK2 and JNK3 inhibitor SC-202671, which resulted in DNA fragmentation during apoptosis, G2/M arrest, phosphorylation of Bcl-2, Mcl-1, and Bim, Δψm loss, and activation of the Bak and caspase cascade.

Biological Activity I Assay Protocols (From Reference)
Targets
JNK3 (pIC50 = 6.7); JNK2 (pIC50 = 6.5)
ln Vitro
JNK inhibitor IX significantly lowers caspase-3 activity in human dermal fibroblasts by preventing JNK activity.[2] By preventing c-ABL from completely dephosphorylating at Ser residues, JNK inhibition by JNK inhibitor IX significantly increases apoptotic death in response to imatinib mesylate (IM).[3]
ln Vivo

Enzyme Assay
JNK2 and JNK3 are specifically inhibited by TCS JNK 5a. With pIC50 values of 6.7, 6.5, <5.0 and <4.8 for JNK3, JNK2, JNK1, and p38α, respectively, TCS JNK 5a demonstrated selective against JNK1 and p38α. TCS JNK 5a also had pIC50 values below 5.0 at EGFR, ErbB2, VegFr2, Src, Tie-2, Alk5, c-Fms, CDK-2, GSK3β and PLK1.
Animal Protocol


References

[1]. Bioorg Med Chem Lett . 2007 Mar 1;17(5):1296-301.

[2]. Toxicol Lett . 2009 Aug 10;188(3):236-42.

[3]. Traffic . 2009 Jun;10(6):637-47.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H16N2OS
Molecular Weight
332.42
Exact Mass
332.10
Elemental Analysis
C, 72.26; H, 4.85; N, 8.43; O, 4.81; S, 9.64
CAS #
312917-14-9
Related CAS #
312917-14-9
Appearance
Solid powder
SMILES
C1CCC2=C(C1)C(=C(S2)NC(=O)C3=CC=CC4=CC=CC=C43)C#N
InChi Key
WQGDQGAFSDMBLA-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H16N2OS/c21-12-17-15-9-3-4-11-18(15)24-20(17)22-19(23)16-10-5-7-13-6-1-2-8-14(13)16/h1-2,5-8,10H,3-4,9,11H2,(H,22,23)
Chemical Name
N-(3-cyano-4,5,6,7-tetrahydro-1-benzothiophen-2-yl)naphthalene-1-carboxamide
Synonyms
JNK Inhibitor IX; CS JNK 5a; TCS-JNK-5a; SC 202671; SC202671; SC-202671
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~20 mg/mL (`60.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0082 mL 15.0412 mL 30.0824 mL
5 mM 0.6016 mL 3.0082 mL 6.0165 mL
10 mM 0.3008 mL 1.5041 mL 3.0082 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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