GlpBio

JAK

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.

JAK 相关产品(162)

  • GC19334 structure
    GC19334Solcitinib
    CAS: 1206163-45-2
    纯度: >99.50%

    A JAK1 inhibitor

  • GC19368 structure
    GC19368Upadacitinib
    CAS: 1310726-60-3
    纯度: >99.50% / >98.00%

    Upadacitinib是一种高效、口服并可逆的选择性 Janus激酶 1 (JAK1) 抑制剂，IC 50 值为0.043μM 。

  • GC19405 structure
    GC19405PF-06700841 P-Tosylate
    CAS: 2140301-96-6
    纯度: >99.50%

    PF-06700841 P-Tosylate是一种强效的双重Janus激酶1（JAK1）和TYK2抑制剂，IC 50 值分别为17nM和23nM。

  • GC19408 structure
    GC19408FM381
    CAS: 2226521-65-7
    纯度: >98.00%

    A potent JAK3 inhibitor

  • GC25168 structure
    GC25168Brepocitinib (PF-06700841)
    CAS: 1883299-62-4

    Brepocitinib (PF-06700841, PF-841) is a potent inhibitor of Tyk2 and Jak1 with IC50s of 23 nM, 17 nM, 77 nM for Tyk2, Jak1 and Jak2 respectively. It has appropriate in-family selectivity against JAK2 and JAK3.

  • GC25869 structure
    GC25869RO495
    CAS: 1258296-60-4

    RO495 (CS-2667) is a potent inhibitor of Non-receptor tyrosine-protein kinase 2 (TYK2).

  • GC25992 structure
    GC25992TG-89
    CAS: 936091-56-4

    TG-89 is an inhibitor of JAK2 with IC50 of 11.2 μM.

  • GC30601 structure
    GC30601Propanamide
    CAS: 916742-11-5

    Propanamide 是一种从专利 WO2012122452A1 化合物 II 中提取的强效选择性 JAK 抑制剂，具有治疗皮肤疾病（如皮肤狼疮）的潜力。

  • GC31659 structure
    GC31659Tyk2-IN-4 (BMS-986165)
    CAS: 1609392-27-9
    纯度: >99.50%

    An allosteric inhibitor of TYK2

  • GC31660 structure
    GC31660Delgocitinib (JTE-052)
    CAS: 1263774-59-9
    纯度: >99.50%

    Delgocitinib (JTE-052) (JTE-052) 是一种特异性 JAK 抑制剂，对 JAK1、JAK2、JAK3 和 Tyk2 的 IC50 分别为 2.8、2.6、13 和 58 nM。

  • GC31668 structure
    GC31668TYK2-IN-2
    CAS: 2098466-94-3
    纯度: >99.50%

    TYK2-IN-2是TYK2的抑制剂，可用于炎症及自身免疫病的研究。

  • GC31677 structure
    GC31677Oclacitinib maleate (PF-03394197 maleate)
    CAS: 1640292-55-2
    纯度: >99.50%

    A JAK family kinase inhibitor

  • GC31866 structure
    GC31866JAK inhibitor 1
    CAS: 2096999-92-5

    JAK inhibitor 1 是从专利 US20170121327A1 化合物实施例 283 中提取的 JAK 抑制剂。

  • GC31902 structure
    GC31902JAK3-IN-6
    CAS: 1443235-95-7
    纯度: >98.00%

    Selective JAK3 inhibitor 1 is an irreversible JAK3 inhibitor with Ki values of 0.07 nM, 320 nM, 740 nM for JAK3, JAK1 and JAK2 respectively. It is also selective over the other kinases possessing a cysteine in the same region as JAK3, such as BMX, EGFR, ITK, and BTK.

  • GC31999 structure
    GC31999JAK-IN-1
    CAS: 1334673-53-8

    JAK-IN-1是JAK1/2/3抑制剂，IC50分别为0.26，0.8和3.2nM。JAK-IN-1对JAK3的选择性比JAK1高。

  • GC32023 structure
    GC32023Abrocitinib (PF-04965842)
    CAS: 1622902-68-4
    纯度: >98.00%

    Abrocitinib (PF-04965842)是一种口服活性且选择性的Janus激酶（JAK）抑制剂，对JAK1和JAK2的IC 50 值分别为29nM和803nM。

  • GC32028 structure
    GC32028BMS-066
    CAS: 914946-88-6

    BMS-066是IKKβ/Tyk2的抑制剂，其IC50值分别为9nM，72nM。

  • GC32052 structure
    GC32052Tyk2-IN-3
    CAS: 1779493-12-7

    Tyk2-IN-3是Tyk2pseudokinase的一个抑制剂，其IC50值为485nM。

  • GC32809 structure
    GC32809Ilginatinib (NS-018)
    CAS: 1239358-86-1
    纯度: >99.00%

    Ilginatinib (NS-018) (NS-018) 是一种高活性且具有口服生物利用度的 JAK2 抑制剂，其 IC50 为 0.72 nM，对 JAK2 的选择性是 JAK1 的 46、54 和 31 倍（IC50，33 nM）， JAK3 (IC50, 39 nM) 和 Tyk2 (IC50, 22 nM)。

  • GC33018 structure
    GC33018Ilginatinib maleate (NS-018 (maleate))
    CAS: 1354799-87-3

    Ilginatinib maleate (NS-018 (maleate)) (NS-018 maleate) 是一种高活性且具有口服生物利用度的 JAK2 抑制剂，其 IC50 为 0.72 nM，对 JAK2 的选择性是对 JAK1 的 46、54 和 31 倍 (IC50 , 33 nM)、JAK3 (IC50, 39 nM) 和 Tyk2 (IC50, 22 nM)。

  • GC33036 structure
    GC33036JAK1-IN-3
    CAS: 2091134-68-6
    纯度: >98.00%

    JAK1-IN-3是一种高选择性、口服活性的Janus激酶1（JAK1）抑制剂，IC 50 值为73nM。

  • GC33037 structure
    GC33037Ilginatinib hydrochloride (NS-018 hydrochloride)
    CAS: 1239358-85-0
    纯度: >98.00%

    Ilginatinib hydrochloride (NS-018 hydrochloride) (NS-018 hydrochloride) 是一种高活性且具有口服生物利用度的 JAK2 抑制剂，其 IC50 为 0.72 nM，对 JAK2 的选择性比 JAK1 高 46、54 和 31 倍 (IC50, 33 nM)、JAK3 (IC50, 39 nM) 和 Tyk2 (IC50, 22 nM)。

  • GC33041 structure
    GC33041Gusacitinib (ASN-002)
    CAS: 1425381-60-7
    纯度: >99.00%

    A dual inhibitor of JAKs and Syk family kinases

  • GC33046 structure
    GC33046JAK3-IN-1
    CAS: 1805787-93-2
    纯度: >99.50%

    JAK3-IN-1是一种有效的JAK3抑制剂,IC50值为4.8nM,也能抑制JAK1(IC50=896nM)和JAK2(IC50=1050nM)。