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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V2962 | Pyridone 6 | 457081-03-7 | Pyridone 6 (also known as P6, CMP 6 or JAK Inhibitor I) is a pan-JAK (Janus-activated kinase) inhibitor with potential anti-AD and anticancer activity. |
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V69738 | QL-1200186 | 2848664-42-4 | QL-1200186 is an orally bioactive and selective TYK2 inhibitor. |
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V51527 | Rovadicitinib | 1948242-59-8 | Rovadicitinib is a JAK inhibitor (antagonist) with IC50 <20 nM. |
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V51525 | Rovadicitinib hydrochloride | 1948242-60-1 | Rovadicitinib HCl is a JAK inhibitor (antagonist) with IC50 <20 nM. |
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V38108 | RSV A405 | 140405-36-3 | RSVA405 is a potent and orally bioactive AMPK activator with EC50 of 1 μM. |
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V0314 | Ruxolitinib (INCB-018424; INC-424) | 941678-49-5 | Ruxolitinib (formerly INC424, INCB18424, INCB018424; trade name Jakafi and Jakavi) is the first-in class, potent, selective, and orally bioavailabe 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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V0076 | Ruxolitinib Phosphate (INC-424, INCB-18424, INCB-018424, Jakafi and Jakavi) | 1092939-17-7 | Ruxolitinib Phosphate (Jakafi and Jakavi), the phosphate salt of ruxolitinib which isalso known as INC424, INCB18424 or INCB018424, is a 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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V0077 | Ruxolitinib sulfate (INC 424, INCB 18424, INCB 018424, Jakafi, Jakavi) | 1092939-16-6 | Ruxolitinib sulfate, the sulfate salt of ruxolitinib which isalso known as Jakafi, Jakavi, INC-424, INCB-18424 or INCB-018424, 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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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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V86065 | Tyk2-IN-14 | 2308520-97-8 |
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