JAK
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Janus kinases (JAKs), belonging to a distinct family of tyrosine kinases, are non-receptor tyrosine kinases that transduce signals of cytokine receptors via diverse signal transduction pathways. Mammalian JAK family consists of four structurally similar members, JAK1, JAK2, JAK3 and Tyrosine kinase 2 (TYK2), which are characterized by containing seven JAK homology (JH) domains. The presence of JH1 and JH2 domains is the most intriguing feature of JAK proteins. JH1 domain is the main catalytic domain; while JH2 is usually considered as a catalytically inactive pseudokinase domain. However, results of recent studies have shown that JH2 acts as a dual-specificity protein kinase to phosphorylate two regulatory sites (Ser523 and Tyr570) in JAK2.
Products Related to JAK(169)
- GC34971(3R,4S)-TofacitinibCAS: 1092578-46-5Purity: >98%
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib.
- GC34972(3S,4R)-TofacitinibCAS: 1092578-48-7Purity: >98%
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib.
- GC34973(3S,4S)-TofacitinibCAS: 1092578-47-6Purity: >99.00%
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib.
- GC36351Itacitinib adipateCAS: 1334302-63-4Purity: >99.00%
Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis.
- GC36365JAK3 covalent inhibitor-1CAS: 2300106-50-5Purity: >98%
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs.
- GC36646Momelotinib MesylateCAS: 1056636-07-7Purity: >98%
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
- GC36882PF-06263276CAS: 1421502-62-6Purity: >99.00%
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively.
- GC37575Ruxolitinib sulfateCAS: 1092939-16-6Purity: >98%
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
- GC39081ReticulineCAS: 485-19-8Purity: >98.00%
Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways.
- GC41329PacritinibCAS: 937272-79-2Purity: >98.00%
FMS-like tyrosine kinase 3 (FLT3) and Janus kinase 2 (JAK2) are tyrosine kinases that mediate cytokine signaling and are frequently mutated in cancers, particularly acute myeloid leukemia.
- GC43406Delphinidin (chloride)CAS: 528-53-0Purity: >98.00%
Delphinidin (chloride) is one of the common monomeric forms of anthocyanins, isolated from berries and red wine.
- GC46148Filgotinib-d4CAS: 2041095-50-3Purity: >99.00%
An internal standard for the quantification of filgotinib
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC34971 | (3R,4S)-Tofacitinib | 1092578-46-5 | >98% | |
(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. | ||||
| GC34972 | (3S,4R)-Tofacitinib | 1092578-48-7 | >98% | |
(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. | ||||
| GC34973 | (3S,4S)-Tofacitinib | 1092578-47-6 | >99.00% | |
(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. | ||||
| GC35554 | Brevilin A | 16503-32-5 | >98.00% | |
A sesquiterpene lactone with anticancer activity | ||||
| GC36351 | Itacitinib adipate | 1334302-63-4 | >99.00% | |
Itacitinib adipate is an orally bioavailable and selective JAK1 inhibitor which has been tested for efficacy and safety in a phase II trial in myelofibrosis. | ||||
| GC36363 | JAK1-IN-7 | 2241039-81-4 | >98% | |
JAK1-IN-7 (JAK1-IN-7) is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect. | ||||
| GC36364 | JAK2-IN-4 | 1438284-00-4 | >98% | |
JAK2-IN-4 (compound 16h) is a selective JAK2/JAK3 inhibitor, with IC50 values of 0.7 nM and 23.2 nM for JAK2 and JAK3, respectively. | ||||
| GC36365 | JAK3 covalent inhibitor-1 | 2300106-50-5 | >98% | |
JAK3 covalent inhibitor-1 is a potent and selective janus kinase 3 (JAK3) covalent inhibitor with an IC50 of 11 nM and shows 246-fold selectivity vs other JAKs. | ||||
| GC36366 | JAK-IN-10 | 916741-98-5 | >98% | |
JAK-IN-10 is a JAK inhibitor. | ||||
| GC36646 | Momelotinib Mesylate | 1056636-07-7 | >98% | |
Momelotinib Mesylate (CYT387 Mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3. | ||||
| GC36783 | NVP-BSK805 dihydrochloride | 1942919-79-0 | >98% | |
A potent, selective JAK2 inhibitor | ||||
| GC36882 | PF-06263276 | 1421502-62-6 | >99.00% | |
PF-06263276 (PF 6263276) is a potent and selective pan-JAK inhibitor, with IC50s of 2.2 nM, 23.1 nM, 59.9 nM and 29.7 nM for JAK1, JAK2, JAK3 and TYK2, respectively. | ||||
| GC37522 | RGB-286638 | 784210-87-3 | >99.50% | |
A multi-kinase inhibitor | ||||
| GC37523 | RGB-286638 free base | 784210-88-4 | >98% | |
A multi-kinase inhibitor | ||||
| GC37575 | Ruxolitinib sulfate | 1092939-16-6 | >98% | |
Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3. | ||||
| GC37846 | Tyk2-IN-7 | 1609391-90-3 | >99.50% | |
Tyk2-IN-7 (Compound 48) is a TYK2 JH2 inhibitor, binds to TYK2 JH2 domain with IC50 and Ki. | ||||
| GC37847 | Tyk2-IN-8 | 2127109-84-4 | >98% | |
Tyk2-IN-8 (Compound 3) is a selective Tyk-2 inhibitor with an IC50 of 5.7 nM for TYK2-JH2. | ||||
| GC37971 | ZM39923 | 273727-89-2 | >98% | |
ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM. | ||||
| GC39081 | Reticuline | 485-19-8 | >98.00% | |
Reticuline shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. | ||||
| GC40761 | VX-509 | 944842-54-0 | >98.00% | |
VX-509 is a selective inhibitor of Janus kinase 3 (JAK3) with a Ki value of 2.5 nM in enzyme assays and an IC50 value of 50-170 nM in cellular assays dependent on JAK3 activity with no measurable activity against other JAK isotypes. | ||||
| GC40791 | MS-1020 | 1255516-86-9 | >95.00% | |
MS-1020 is a cell-permeable inhibitor of janus kinase 3 (JAK3), strongly inhibiting constitutive autophosphorylation of JAK3 in L540 cells when used at 30-50 μM. | ||||
| GC41329 | Pacritinib | 937272-79-2 | >98.00% | |
FMS-like tyrosine kinase 3 (FLT3) and Janus kinase 2 (JAK2) are tyrosine kinases that mediate cytokine signaling and are frequently mutated in cancers, particularly acute myeloid leukemia. | ||||
| GC43406 | Delphinidin (chloride) | 528-53-0 | >98.00% | |
Delphinidin (chloride) is one of the common monomeric forms of anthocyanins, isolated from berries and red wine. | ||||
| GC46148 | Filgotinib-d4 | 2041095-50-3 | >99.00% | |
An internal standard for the quantification of filgotinib | ||||