420099

JAK Inhibitor I

≥98% (HPLC), solid, JAK inhibitor, Calbiochem^®

• Sinónimos: JAK Inhibitor I, 2-(1,1-Dimethylethyl)-9-fluoro-3,6-dihydro-7H-benz[h]-imidaz[4,5-f]isoquinolin-7-one, Pyridone 6, P6, DBI, JAK1 Inhibitor I, JAK2 Inhibitor I, JAK3 Inhibitor X
• Fórmula empírica (notación de Hill): C₁₈H₁₆FN₃O
• Número de CAS: 457081-03-7
• Peso molecular: 309.34
• Número MDL: MFCD17019334
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nombre del producto: JAK Inhibitor I, JAK Inhibitor I, CAS 457081-03-7, is a potent, reversible, cell-permeable, and ATP-competitive inhibitor of JAK 1 (IC₅₀ = 15 nM), JAK2 (IC₅₀ = 1 nM), JAK3 (K_i = 5 nM) and Tyk2 (IC₅₀ = 1 nM).
• Nivel de calidad: 100
• Ensayo: ≥98% (HPLC)
• Formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: off-white
• solubilidad: DMSO: 5 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: −20°C
• cadena SMILES: Fc1cc2c(c3[nH]c(nc3c4c2c(ncc4)O)C(C)(C)C)cc1
• InChI: 1S/C18H16FN3O/c1-18(2,3)17-21-14-10-5-4-9(19)8-12(10)13-11(15(14)22-17)6-7-20-16(13)23/h4-8H,1-3H3,(H,20,23)(H,21,22)
• Clave InChI: VNDWQCSOSCCWIP-UHFFFAOYSA-N

Descripción

Descripción general

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC₅₀ = 15 nM for murine JAK1), JAK2 (IC₅₀ = 1 nM), JAK3 (K_i = 5 nM), and Tyk2 (IC₅₀ = 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5, and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401).

A potent, reversible, cell-permeable, and ATP-competitive inhibitor of Janus protein tyrosine kinases (JAKs). Displays potent inhibitory activity against JAK1 (IC₅₀ = 15 nM for murine JAK1), JAK2 (IC₅₀ = 1 nM), JAK3 (K_i = 5 nM), and Tyk2 (IC₅₀ = 1 nM). Inhibits other kinases at much higher concentrations. Shown to inhibit IL2- and IL4-dependent proliferation of CTLL cells and block the phosphorylation of STAT5; and further induce growth inhibition of multiple myeloma cells expressing activated JAKs and STAT3, unlike AG 490 (Cat. No. 658401). A 10 mM (500 µg/162 µl) solution of JAK Inhibitor I (Cat. No. 420097) in DMSO is also available.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
murine JAK1

Product competes with ATP.

Reversible: yes

Target IC₅₀: 15 nM against murine JAK1; 1 nM against JAK2; 1 nM against Tyk2

Target K_i: 5 nM against JAK3

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Otras notas

Pedranzini, L., et al. 2006. Cancer Res.66, 9714.
Lucet, I.S., et al. 2005. Blood107, 176.
Thompson, J.E., et al. 2002. Bioorg. Med. Chem. Lett.12, 1219.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable