Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway.Members of the type I and type II cytokine receptor families depend on the JAK family of tyrosine kinases to phosphorylate and activate downstream proteins involved in their signal transduction pathways because they lack catalytic kinase activity.The receptors have two intracellular signal-transducing domains because they are paired polypeptides. Each intracellular domain contains a proline-rich region called a box1/box2 region that is close to the cell membrane and where JAKs bind. The two JAKs are brought close enough to phosphorylate one another after the receptor undergoes a conformational change following association with the corresponding cytokine or ligand. By further phosphorylating and activating STAT transcription factors, JAK autophosphorylation causes a conformational change within itself, enabling it to transduce the intracellular signal. When STATs are activated, they separate from their receptor and coalesce into dimers before moving into the cell nucleus, where they control the transcription of particular genes.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
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V0337 | S-Ruxolitinib (INCB-018424) | 941685-37-6 | S-Ruxolitinib, the S-enantiomer of ruxolitinib which is also known as INC424 and INCB18424 or INCB018424,is the first-in class, potent, selective, and orally bioavailable JAK1/2 (Janus-associated kinase) inhibitor with IC50 of 3.3 nM/2.8 nM in cell-free assays, it exhibits >130-fold selectivity for JAK1/2 versus JAK3. |
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V3369 | SAR-20347 | 1450881-55-6 | SAR-20347 is a novel and potent small molecule inhibitor with specificity for JAK1 and tyrosine kinase 2 (TYK2) over other JAK family members. |
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V51516 | SJ-1008030 | 2863634-96-0 | SJ1008030 (compound 8) is a JAK2 PROTAC that selectively degrades JAK2. |
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V53150 | SJ10542 | 2789678-92-6 | SJ10542 is a potent and specific JAK2/3-directed phenylglutarimide (PG)-PROTAC with DC50s of 14, 11, and 24 nM for JAK2, JAK3, and JAK2-fusion ALL, respectively. |
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V2959 | Solcitinib | 1206163-45-2 | Solcitinib (formerly GSK2586184; GSK-2586184A; GLPG-0778;GLPG0778) is a potent, selective, and orally bioavailable Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis. |
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V15932 | TCJL-37 | 1258294-34-6 | TCJL37 is a potent, orally bioactive and selective TYK2 inhibitor (antagonist) with Ki of 1.6 nM. |
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V0315 | Tofacitinib (CP690550) Citrate | 540737-29-9 | Tofacitinib citrate (formerly CP-690550 citrate), the citrate salt of tofacitinib (tasocitinib or CP 690550, brand Xeljanz), is a novel, potent andorally bioavailable inhibitor of JAK3 (Janus-Associated kinase) with IC50 of 1 nM in cell-free assays. |
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V0342 | Tofacitinib (CP690550; tasocitinib) | 477600-75-2 | Tofacitinib (also known as tasocitinib or CP-690550, sold under the brandXeljanz),is a novel and potent inhibitor of JAK3 (Janus-Associated kinase) with potential anti-inflammatory activity. |
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V51510 | TUL-01101 | 2411222-97-2 | TUL01101 is a specific and orally bioactive JAK1 inhibitor (antagonist) with IC50s of 3, 37, 1517 and 36 nM for JAK1, JAK2, JAK3 and TYK2 respectively. |
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V35164 | TX-1123 | 157397-06-3 | TX-1123 is a potent protein tyrosine kinase (PTK) inhibitor targeting Src, eEF2-K, PKA and EGFR-K/PKC. |
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V56092 | TYK2 JH2-IN-1-d3 | 2376999-19-6 | TYK2 JH2-IN-1-d3 is a deuterated, orally bioactive and selective TYK2 inhibitor (compound 4h) targeting the JH2 domain (IC50=0.1 nM). |
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V35163 | Tyrphostin AG213 (AG213) | 122520-86-9 | Tyrphostin AG213 (AG213) is an epidermal growth factor receptor (EGFR) protein tyrosine kinase inhibitor (IC50=0.85 μM). |
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V4510 | Upadacitinib tartrate | 1607431-21-9 | Upadacitinib tartrate (formerly ABT494; ABT-494; rinvoq), the tartrate salt ofUpadacitinib, is a novel, potent and selective Janus kinase (JAK) 1 inhibitor approved in 2019 for the treatment of rheumatoid arthritis. |
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V51514 | VVD-118313 | 2875046-27-6 | VVD-118313 (compound 5a) is a potent selective JAK1. |
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V3972 | WHI-P97 | 211555-05-4 | WHI-P97 is a novel, rationally designed, and potent inhibitor of Janus kinase (JAK)-3 with an estimated Ki value of 0.09 μM in modeling studies and a measured IC50 value of 2.5 μM in EGFR kinase inhibition assays. |
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V0330 | XL019 | 945755-56-6 | XL019 is a novel,potent and selective and orally bioavailable inhibitor of Janus kinase-JAK2 with potential antitumor activity. |
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V50938 | Zasocitinib (NDI-034858) | 2272904-53-5 | Zasocitinib (NDI-034858) is a Tyk2 inhibitor that targets the JH2 domain of Tyk2 with a binding constant Kd <200 pM. |
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V0329 | ZM 39923 HCl | 1021868-92-7 | ZM 39923 HCl, the hydrochloride salt of ZM-39923,is a novel and potent inhibitor of Janus kinase-JAK1/3 with potential anti-inflammatory activity. |
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V51523 | ZT-55 | 2138488-38-5 | ZT55 is an effective and selective JAK2 mold with IC50 of 0.031 μM. |
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