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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(190)

  • GC10341 structure
    GC10341Peficitinb (ASP015K, JNJ-54781532)
    CAS: 944118-01-8
    Purity: >98.00%

    Peficitinb(ASP015K, JNJ-54781532)(ASP015K)는 JAK1, JAK2, JAK3 및 Tyk2에 대해 IC50이 각각 3.9, 5.0, 0.7 및 4.8nM인 경구 활성 JAK 억제제입니다.

  • GC10638 structure
    GC10638AT9283
    CAS: 896466-04-9
    Purity: >99.50%

    A broad spectrum kinase inhibitor

  • GC10770 structure
    GC10770Decernotinib(VX-509)
    CAS: 944842-54-0
    Purity: >98.00%

    Decernotinib(VX-509)는 강력한 경구 활성 JAK3 억제제로 JAK3, JAK1, JAK2 및 TYK2에 대해 각각 2.5, 11, 13 및 11nM의 Kis를 나타냅니다.

  • GC11209 structure
    GC11209Cerdulatinib (PRT062070)
    CAS: 1198300-79-6
    Purity: >99.50%

    세둘라티닙(PRT062070)(PRT062070)은 IC50이 0.5nM인 선택적 Tyk2 억제제입니다. 세둘라티닙(PRT062070)(PRT062070)은 또한 JAK1, 2, 3 및 SYK에 대해 각각 IC50이 12, 6, 8 및 32인 이중 JAK 및 SYK 억제제입니다.

  • GC11525 structure
    GC11525Pyridone 6
    CAS: 457081-03-7
    Purity: >98.50%

    Pyridone 6은 가역적이고 세포 투과성이 있는 판-자누스 활성효소 (JAK) 억제제이다. Pyridone 6은 JAK1/2/3 (IC 50 =15nM, 1nM, 5nM) 및 TYK2 (IC 50 =1nM)의 활성을 억제해서 JAK-STAT 신호 전달을 차단한다.

  • GC11572 structure
    GC11572Bardoxolone methyl
    CAS: 218600-53-4
    Purity: >98.50%

    Bardoxolone methyl은 핵 인자 적혈구 2 관련 인자 2(Nrf2)에 의해 매개되는 항산화 및 항염증 반응의 효과적인 활성제이고 NF-κB 경로의 억제제이다 .

  • GC11652 structure
    GC11652CHZ868
    CAS: 1895895-38-1
    Purity: >99.00%

    CHZ868은 EPOR JAK2 WT Ba/F3 세포에서 IC50이 0.17μM인 II형 JAK2 억제제입니다.

  • GC12064 structure
    GC12064SB1317
    CAS: 937270-47-8
    Purity: >99.50%

    A multi-kinase inhibitor

  • GC12083 structure
    GC12083CEP-33779
    CAS: 1257704-57-6
    Purity: >99.00%

    A potent, orally available inhibitor of JAK2

  • GC12454 structure
    GC12454BMS-911543
    CAS: 1271022-90-2
    Purity: >98.00%

    A potent, selective JAK2 inhibitor

  • GC12504 structure
    GC12504AZD1480
    CAS: 935666-88-9
    Purity: >98.00%

    AZD1480은 JAK 억제제(JAK1: IC50 = 1.3nM; JAK2: IC50 = 0.4nM)이다.

  • GC13229 structure
    GC13229NVP-BSK805
    CAS: 1092499-93-8
    Purity: >98.00%

    A potent, selective JAK2 inhibitor

  • GC13433 structure
    GC13433AZ 960
    CAS: 905586-69-8
    Purity: >98.00%

    A JAK2 inhibitor

  • GC13826 structure
    GC13826JAK2 Inhibitor V, Z3
    CAS: 195371-52-9
    Purity: >98.00%

    A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK

  • GC13830 structure
    GC13830Baricitinib phosphate
    CAS: 1187595-84-1
    Purity: >99.50%

    A JAK1 and JAK2 inhibitor

  • GC13848 structure
    GC13848LY2784544
    CAS: 1229236-86-5
    Purity: >99.50%

    Potent inhibitor of JAK2

  • GC14191 structure
    GC14191Ruxolitinib (INCB18424)
    CAS: 941678-49-5
    Purity: >98.00%

    Ruxolitinib (INCB018424)은 억제제로서 JAK1과 JAK2 Janus 관련 효소를 각각 3.3 nM 및 2.8 nM의 IC50 값으로 억제한다.

  • GC14245 structure
    GC14245ZM 39923 HCl
    CAS: 1021868-92-7
    Purity: >99.50%

    A potent inhibitor of JAK3

  • GC14324 structure
    GC14324TG101348 (SAR302503)
    CAS: 936091-26-8
    Purity: >99.50%

    TG101348 (SAR302503)는 IC 50 값이 3 nM인 선택적 소분자 JAK2 억제제이다.

  • GC14327 structure
    GC14327XL019
    CAS: 945755-56-6
    Purity: >98.00%

    A potent, bioavailable JAK2 inhibitor

  • GC14671 structure
    GC14671JANEX-1
    CAS: 202475-60-3
    Purity: >98.00%

    A selective JAK3 inhibitor

  • GC14676 structure
    GC14676Pacritinib (SB1518)
    CAS: 937272-79-2
    Purity: >98.00%

    파크리티닙(SB1518)(SB1518)은 야생형 JAK2(IC50=23nM) 및 JAK2V617F 돌연변이(IC50=19nM) 둘 다의 강력한 억제제입니다. 파크리티닙(SB1518)은 또한 FLT3(IC50=22nM) 및 돌연변이 FLT3D835Y(IC50=6nM)를 억제합니다.

  • GC14844 structure
    GC14844Baricitinib (LY3009104, INCB028050)
    CAS: 1187594-09-7
    Purity: >99.50%

    Baricitinib (LY3009104, INCB028050)는 JAK1 및 JAK2에 대한 IC₅₀가 각각 5.9 nM, 5.7 nM인 강력한 경구용 억제제이다.

  • GC14857 structure
    GC14857LFM-A13
    CAS: 244240-24-2
    Purity: >99.50%

    LFM-A13은 강력한 BTK, JAK2, PLK 억제제이며 2.5μM, 10μM 및 61μM의 IC50으로 재조합 BTK, Plx1 및 PLK3을 억제합니다. LFM-A13은 JAK1 및 JAK3, Src 계열 키나제 HCK, EGFR 및 IRK에 영향을 미치지 않습니다.