Molecular structure of Janex-1, CAS Number: 202475-60-3
Janex-1 (CAS 202475-60-3)
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Alternate Names:
WHI-P131
Application:
Janex-1 is a selective inhibitor of tyrosine kinase activity of JAK3
CAS Number:
202475-60-3
Purity:
≥98%
Molecular Weight:
297.3
Molecular Formula:
C16H15N3O3
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Janex-1 is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (Janus family kinase 3 IC50 = 78 muM). Janex-1 has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases. Janex-1 acts as a potent inhibitor of glioblastoma cell adhesion and migration and is also reported to block thrombin-induced platelet aggregation.
Janex-1 (CAS 202475-60-3) References
- CYP1A-mediated metabolism of the Janus kinase-3 inhibitor 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline: structural basis for inactivation by regioselective O-demethylation. | Uckun, FM., et al. 2002. Drug Metab Dispos. 30: 74-85. PMID: 11744615
- Janus kinase 3 inhibitor WHI-P131/JANEX-1 prevents graft-versus-host disease but spares the graft-versus-leukemia function of the bone marrow allografts in a murine bone marrow transplantation model. | Uckun, FM., et al. 2002. Blood. 99: 4192-9. PMID: 12010825
- Targeting JAK3 with JANEX-1 for prevention of autoimmune type 1 diabetes in NOD mice. | Cetkovic-Cvrlje, M., et al. 2003. Clin Immunol. 106: 213-25. PMID: 12706408
- Prevention of islet allograft rejection in diabetic mice by targeting Janus Kinase 3 with 4-(4'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (JANEX-1). | Cetkovic-Cvrlje, M., et al. 2003. Arzneimittelforschung. 53: 648-54. PMID: 14558439
- Targeting mast cells in endometriosis with janus kinase 3 inhibitor, JANEX-1. | D'Cruz, OJ. and Uckun, FM. 2007. Am J Reprod Immunol. 58: 75-97. PMID: 17631002
- Effect of targeting janus kinase 3 on the development of intestinal tumors in the adenomatous polyposis coli(min) mouse model of familial adenomatous polyposis. | Uckun, FM., et al. 2007. Arzneimittelforschung. 57: 320-9. PMID: 17688077
- Anti-inflammatory activity profile of JANEX-1 in preclinical animal models. | Uckun, FM., et al. 2008. Bioorg Med Chem. 16: 1287-98. PMID: 18024136
- Targeting JAK3 tyrosine kinase-linked signal transduction pathways with rationally-designed inhibitors. | Uckun, FM., et al. 2007. Anticancer Agents Med Chem. 7: 612-23. PMID: 18045056
- JANEX-1, a JAK3 inhibitor, protects pancreatic islets from cytokine toxicity through downregulation of NF-kappaB activation and the JAK/STAT pathway. | Lv, N., et al. 2009. Exp Cell Res. 315: 2064-71. PMID: 19414010
- Janex-1, a JAK3 inhibitor, ameliorates tumor necrosis factor-α-induced expression of cell adhesion molecules and improves myocardial vascular permeability in endotoxemic mice. | Lee, JE., et al. 2012. Int J Mol Med. 29: 864-70. PMID: 22344597
- Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice. | Oh, YB., et al. 2013. Exp Mol Med. 45: e23. PMID: 23680658
- IL21R expressing CD14+CD16+ monocytes expand in multiple myeloma patients leading to increased osteoclasts. | Bolzoni, M., et al. 2017. Haematologica. 102: 773-784. PMID: 28057743
- JANEX-1 improves acute pulmonary embolism through VEGF and FAK in pulmonary artery smooth muscle cells. | Pan, L., et al. 2020. Exp Biol Med (Maywood). 245: 1395-1403. PMID: 32664806
- Janus Kinase 3 phosphorylation and the JAK/STAT pathway are positively modulated by follicle-stimulating hormone (FSH) in bovine granulosa cells. | Zareifard, A., et al. 2023. BMC Mol Cell Biol. 24: 21. PMID: 37337185
Inhibitor of:
3BP1, C-MIP, GDNF, JAK3, and SH2-B.Activator of:
Tec.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Janex-1, 1 mg | sc-205354 | 1 mg | $36.00 | |||
Janex-1, 5 mg | sc-205354A | 5 mg | $153.00 |