420104
JAK3 Inhibitor II
The JAK3 Inhibitor II, also referenced under CAS 211555-04-3, controls the biological activity of JAK3. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
동의어(들):
JAK3 Inhibitor II, 4-[(3ʹ-Bromo-4ʹ-hydroxyphenyl)amino]-6,7-dimethoxyquinazoline, WHI-P154
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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C16H14BrN3O3
CAS 번호:
Molecular Weight:
376.20
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
SMILES string
Brc1c(ccc(c1)Nc2ncnc3c2cc(c(c3)OC)OC)O
InChI
1S/C16H14BrN3O3/c1-22-14-6-10-12(7-15(14)23-2)18-8-19-16(10)20-9-3-4-13(21)11(17)5-9/h3-8,21H,1-2H3,(H,18,19,20)
InChI key
CBIAKDAYHRWZCU-UHFFFAOYSA-N
assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
pale yellow
solubility
DMSO: 100 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
A potent, cell-permeable, reversible, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 5.6 µM). Has no effect on either JAK1 or JAK2. Has also been shown to prevent the ionizing radiation-induced activation of c-Jun in DT-40 cells. Also acts as a potent inhibitor of glioblastoma cell adhesion and migration.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
JAK-3
JAK-3
Product competes with ATP.
Reversible: yes
Target IC50: 5.6 µM against JAK3
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.
Other Notes
Ghosh, S., et al. 2001. Acta Crystallogr. C.57, 76.
Sudbeck, E.A., et al. 1999. Clin. Cancer Res. 5, 1569.
Goodman, P.A., et al. 1998. J. Biol. Chem. 273, 17742.
Narla, R.K., et al. 1998. Clin Cancer Res.4, 2463.
Sudbeck, E.A., et al. 1999. Clin. Cancer Res. 5, 1569.
Goodman, P.A., et al. 1998. J. Biol. Chem. 273, 17742.
Narla, R.K., et al. 1998. Clin Cancer Res.4, 2463.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
저장 등급
11 - Combustible Solids
wgk
WGK 3
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
R K Narla et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 4(10), 2463-2471 (1998-10-31)
Glioblastoma multiforme is a highly invasive primary brain tumor with a disappointingly high local recurrence rate and mortality despite intensive multimodality treatment programs. Therefore, new agents that are capable of inhibiting the infiltration of normal brain parenchyma by glioblastoma cells
S Ghosh et al.
Acta crystallographica. Section C, Crystal structure communications, 57(Pt 1), 76-78 (2001-02-15)
The title compounds, C16H15BrN3(O3)(+).Cl(-).CH4O (WHI-P154) and C16H16N3(O3)(+).Cl(-) (WHI-P180), are potent inhibitors [WHI-P154 with IC50 = 5.6 microM and WHI-P180 with IC50 = 4.0 microM for epidermal growth factor receptor (EGFR) kinase inhibition] of the EGFR tyrosine kinase as well as
E A Sudbeck et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 5(6), 1569-1582 (1999-07-02)
A novel homology model of the kinase domain of Janus kinase (JAK) 3 was used for the structure-based design of dimethoxyquinazoline compounds with potent and specific inhibitory activity against JAK3. The active site of JAK3 in this homology model measures
P A Goodman et al.
The Journal of biological chemistry, 273(28), 17742-17748 (1998-07-04)
Exposure of B-lineage lymphoid cells to ionizing radiation induces an elevation of c-jun proto-oncogene mRNA levels. This signal is abrogated by protein-tyrosine kinase (PTK) inhibitors, indicating that activation of an as yet unidentified PTK is mandatory for radiation-induced c-jun expression.
국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| 420104-5MGCN | 04055977187908 |
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