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Merck

420099

JAK Inhibitor I

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

동의어(들):

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

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크기 선택

제품정보 (DICE 배송 시 비용 별도)

실험식(Hill 표기법):
C18H16FN3O
CAS 번호:
457081-03-7
Molecular Weight:
309.34
MDL number:
MFCD17019334
UNSPSC Code:
12352200
NACRES:
NA.77

주요 문서

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제품 이름

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 (Ki = 5 nM) and Tyk2 (IC50 = 1 nM).

SMILES string

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)

InChI key

VNDWQCSOSCCWIP-UHFFFAOYSA-N

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

color

off-white to light brown

관련 카테고리

Biochem/physiol Actions

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 Ki: 5 nM against JAK3

Disclaimer

Toxicity: Standard Handling (A)

General description

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 (Ki = 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 (Ki = 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.

Other Notes

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.

Packaging

Packaged under inert gas

Preparation Note

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

Legal Information

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

저장 등급

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

시험 성적서(COA)

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An Introduction to Inhibitors and Their Biological Applications - 1st Edition

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JAK/STAT Signaling Research Focus

The Janus kinase (JAK)/signal transducers and activators of transcription (STAT) signaling pathway plays an important role in cell proliferation, cell differentiation, cell migration, and cell death. It is the principal signaling mechanism for a variety of cytokines and growth factors. Constitutive activation or dysregulation of JAK/STAT signaling can result in inflammatory disease, erythrocytosis, gigantism, and leukemia.

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국제 무역 품목 번호

SKUGTIN
420099-1MGCN04055977187878
420099-500UGCN04055977187885

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