JAK-STAT
JAKs (Janus Kinase; EC 2.7.10.2; 4 types identified) and STATs (Signal Transducer and Activator of Transcription; 7 types identified) are critical components of many cytokine receptor systems, regulating growth, survival, differentiation and pathogen resistance. (Cytokine) receptor-bound STATs phosphorylated by JAKs dimerize and translocate into the nucleus to regulate target gene transcription. In most cases, a specific JAK-STAT combination has been paired with a specific member of the cytokine receptor family, and this information translated into cell-type specific patterns of cytokine responsiveness and gene expression. Members of the suppressor of cytokine signaling (SOCS) protein family dampen receptor signaling via homologous or heterologous feedback regulation[1],[2]. Consequently, Janus kinase mutations are major molecular events in human hematological malignancies[3].
[1] The JAK-STAT Signaling Pathway: Input and Output Integration. P.J. Murray. J. Immunol. 2007, 178, 2623-2629.
[2] A Road Map for Those Who Don't Know JAK-STAT. D.S. Aaronson, C.M. Horvath. Science 2002, 296, 1653-1655.
[3] Cytokine receptor signaling through the Jak-Stat-Socs pathway in disease. O'Sullivan LA, Liongue C, Lewis RS, Stephenson SE, Ward AC. Mol. Immunol. 2007, 44, 2497–506.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 2496 | 2,5-Dimethylcelecoxib | Celecoxib analog with anti-tumor properties, lacking COX-2 inhibitory activity | €75.00 | |
| 3040 | Abivertinib | Potent oral, irreversible, third-generation EGFR TKI with selectivity for mutant EGFRs | €95.00 | |
| 1653 | AEE 788 | EGFR, ErbB2 and VEGFR tyrosine kinase inhibitor | €80.00 | |
| 1378 | AG 490 | JAK2 inhibitor | €65.00 | |
| 1992 | AS 1517499 | Potent and selective STAT6 inhibitor | €130.00 | |
| 3997 | ASN-002 | Potent dual inhibitor of SYK and pan-JAK kinases | Inquire | |
| 1986 | AST 1306 tosylate | ErbB2 and EGFR inhibitor | €90.00 | |
| 2219 | AT 9283 | Multitargeted kinase inhibitor (Aurora A/B, JAK2/3, and BCR-Abl) | €85.00 | |
| 5051 | Axon Ligands™ Cell signaling and Oncology compound library | Axon Ligands™ Cell signaling and Oncology compound library | Inquire | |
| 1778 | AZ 960 | JAK2 inhibitor | €95.00 | |
| 3855 | AZD-4205 | Selective and ATP-competitive inhibitor of JAK1 | Inquire | |
| 2795 | AZD1208 | Pim kinase inhibitor | €70.00 | |
| 2563 | AZD3759 | Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor | €85.00 | |
| 2342 | AZD9291 | Potent oral, irreversible, third-generation EGFR TKI with selectivity for mutant EGFRs | €95.00 | |
| 2981 | B106 | Potent and selective PKC-δ inhibitor | €135.00 | |
| 1955 | Baricitinib | Inhibitor of JAK1 and JAK2 | €70.00 | |
| 1544 | BIBW 2992 | EGFR and ErbB-2/HER2 tyrosine kinase inhibitor | €50.00 | |
| 3853 | BMS-599626 | Potent and selective EGFR and ErbB2 inhibitor | Inquire | |
| 3813 | BMS-911543 | Potent, selective and orally active inhibitor of JAK2 | Inquire | |
| 3786 | BP-1-102 | Orally bioavailable STAT3 inhibitor | €90.00 | |
| 2489 | Brassinin | Dual IDO1/STAT3 inhibitor with antifungal and anticancer activity | €75.00 | |
| 3671 | CEP-33779 | Potent, selective and orally bioavailable JAK2 inhibitor | €95.00 | |
| 2775 | Cerdulatinib | Orally active dual Syk/JAK inhibitor | €85.00 | |
| 1433 | CI 1033 | EGFR tyrosine kinase inhibitor | €60.00 | |
| 1338 | CP 690550 | JAK3 inhibitor | €60.00 | |
| 1537 | CP 724714 | ErbB-2/HER2 kinase inhibitor | €80.00 | |
| 2455 | CU-T12-9 | Selective TLR1/TLR2 agonist that facilitates the TLR1/2 complex formation | €120.00 | |
| 3923 | CUDC-305 | Orally bioavailable inhibitor of Heat Shock Proteins | Inquire | |
| 2305 | CX 6258 hydrochloride | Pim kinase inhibitor | €99.00 | |
| 3235 | Dacomitinib | Potent irreversible pan-HER inhibitor | €60.00 | |