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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)

  • GC46191 structure
    GC46191Oclacitinib-13C-d3
    CAS: 2750534-84-8
    Purity: >99.00%

    A neuropeptide with diverse biological activities

  • GC46503 structure
    GC465032-NP
    CAS: 65182-56-1
    Purity: >99.50%

    2-NP is a cell-penetrating, selective signal transduction and transcription activator 1 (STAT1) transcription enhancer.

  • GC47450 structure
    GC47450IL-4 Inhibitor
    CAS: 1332184-63-0
    Purity: >98.00%

    IL-4 Inhibitor (compound 52) is an IL-4 inhibitor, with an EC50 of 1.81 μM.

  • GC49692 structure
    GC49692Tofacitinib-d3 (citrate)
    Purity: >99.00%

    An internal standard for the quantification of tofacitinib

  • GC50003 structure
    GC50003AG 490
    CAS: 133550-30-8
    Purity: >98%

    EGFR-kinase inhibitor. Also JAK2, JAK3 inhibitor

  • GC50066 structure
    GC50066Atiprimod dihydrochloride
    CAS: 130065-61-1
    Purity: >98%

    JAK2 inhibitor

  • GC50480 structure
    GC50480PF 06651600 malonate
    CAS: 2140301-97-7
    Purity: >98%

    Potent and selective JAK3 inhibitor

  • GC60161 structure
    GC60161Fedratinib hydrochloride hydrate
    CAS: 1374744-69-0
    Purity: >98.00%

    Fedratinib hydrochloride hydrate is an effective, selective, ATP competitive and orally active JAK2 inhibitor, and the IC 50 values for both JAK2 and JAK2V617F kinases are 3nM.

  • GC61807 structure
    GC61807(E/Z)-AG490
    CAS: 134036-52-5
    Purity: >98.00%

    (E/Z)-AG490 ((E/Z)-Tyrphostin AG490) is a racemic compound of (E)-AG490 and (Z)-AG490 isomers. (E)-AG490 is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.

  • GC61995 structure
    GC61995PKCβ inhibitor 1
    CAS: 257879-35-9
    Purity: >98.00%

    PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).

  • GC62112 structure
    GC62112Zotiraciclib
    CAS: 1204918-72-8
    Purity: >99.00%
  • GC62130 structure
    GC62130(2R,5S)-Ritlecitinib
    CAS: 1792180-79-0
    Purity: >98.50%

    (2R,5S)-Ritlecitinib ((2R,5S)-PF-06651600) is a potent and selective JAK3 inhibitor (IC50=144.8 nM) extracted from patent US20150158864A1, example 68.

  • GC62233 structure
    GC622332,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide
    CAS: 1258292-64-6
    Purity: >98.50%

    GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively.

  • GC62246 structure
    GC62246G5-7
    CAS: 939681-36-4
    Purity: >99.50%

    G5-7, an orally active and allosteric JAK2 inhibitor, selectively inhibits JAK2 mediated phosphorylation and activation of EGFR (Tyr1068) and STAT3 by binding to JAK2. G5-7 induces cell cycle arrest, apoptosis and possesses antiangiogenic effect. G5-7 has the potential for glioma study.

  • GC62313 structure
    GC62313Izencitinib
    CAS: 2051918-33-1
    Purity: >99.00%

    Izencitinib (TD-1473) is an orally active, non-selective and gut-restricted JAK inhibitor.

  • GC62491 structure
    GC62491BMS-986202
    CAS: 1771691-34-9
    Purity: >99.00%

    BMS-986202 is a potent, selective and orally active Tyk2 inhibitor that binds to Tyk2 JH2 with an IC50 of 0.19 nM and a Ki of 0.02 nM.

  • GC62500 structure
    GC62500JAK2-IN-7
    CAS: 2593402-36-7
    Purity: >99.00%

    JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.

  • GC62665 structure
    GC62665JAK2/FLT3-IN-1 TFA
    Purity: >98.50%

    JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.

  • GC62908 structure
    GC62908Coumermycin A1
    CAS: 4434-05-3
    Purity: >97.00%

    Coumermycin A1 is an aminocoumarin antibiotic produced by Streptomyces and acts as a DNA gyrase inhibitor.

  • GC63029 structure
    GC63029JAK1-IN-8
    CAS: 1973485-18-5
    Purity: >98.00%

    JAK1-IN-8, a potent JAK1 inhibitor (IC50<500 nM), compound 28, extracted from patent WO2016119700A1.

  • GC63309 structure
    GC63309Ilunocitinib
    CAS: 1187594-14-4
    Purity: >98%

    Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1).

  • GC63416 structure
    GC63416Itacnosertib
    CAS: 1628870-27-8
    Purity: >98%

    Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871.

  • GC63448 structure
    GC63448JAK-IN-14
    CAS: 1973485-06-1
    Purity: >98.50%

    JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM.

  • GC63864 structure
    GC63864(E/Z)-Zotiraciclib hydrochloride
    CAS: 1321626-25-8
    Purity: >98%

    (E/Z)-Zotiraciclib ((E/Z)-TG02) hydrochloride is a potent CDK2, JAK2, and FLT3 inhibitor.