GlpBio

MAP4K

MAP4Ks (Mitogen-activated protein kinase kinase kinase kinases) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4K family members, including Hematopoietic progenitor kinase 1 (HPK1/MAP4K1), Germinal centre kinase (GCK/MAP4K2), Germinal centre kinase-like kinase (GLK/MAP4K3), HPK/GCK-like kinase (HGK/MAP4K4), Misshapen-like kinase 1 (MINK1/MAP4K6) and TRAF2 and NCK interacting kinase (TNIK/MAP4K7), as potent LATS1/2-activating kinases.

Overexpression or deletion of MAP4Ks affects the phosphorylation and activity of Large tumor suppressor 1/2 (LATS1/2, homologues of Wts) and Yes-associated protein (YAP) /transcriptional co-activator with PDZ-binding motif (TAZ). By acting in a LATS-dependent, but Mammalian Ste20-like kinases 1/2 (MST1/2, homologues of Hpo)-independent manner, MAP4Ks restrict the activity of YAP/TAZ by promoting their phosphorylation and inhibiting target gene expression. MAP4Ks are components of the Hippo pathway by directly phosphorylating and activating the LATS1/2 kinases.MAP4K2/4/6 and MST1/2 both belong to the STE20-like kinase family, and their kinase domains are highly homologous to one another. MAP4K4 acts through LATS to inhibit YAP and cell proliferation.

MAP4K 相关产品(25)

  • GC12151 structure
    GC12151B-Raf inhibitor
    CAS: 1315330-11-0
    纯度: >98.50%

    B-Raf inhibitor 是一种有效的双重 TGFβ-activated kinase 1 (TAK1) 和 mitogen-activated protein kinase kinase kinase 2 (MAP4K2) 抑制剂，IC50 分别为 41.1 nM 和 18.2 nM。

  • GC13514 structure
    GC13514NG25
    CAS: 1315355-93-1
    纯度: >98.00%

    NG25是一种强效且可渗透细胞的TGF-β-活化蛋白激酶1（TAK1）和丝裂原激活蛋白激酶激酶激酶激酶2（MAP4K2）抑制剂，IC 50 值分别为149nM和21.7nM。

  • GC18257 structure
    GC18257GNE-495
    CAS: 1449277-10-4
    纯度: >99.50%

    An orally bioavailable, potent, and selective MAP4K4 inhibitor

  • GC19260 structure
    GC19260NCB-0846
    CAS: 1792999-26-8
    纯度: >98.00%

    A TNIK inhibitor

  • GC25289 structure
    GC25289CompK

    CompK (compound K), a potent and selective hematopoietic progenitor kinase 1 (HPK1 or MAP4K1) small molecule inhibitor, significantly improves human T-cell functions, with enhanced T-cell receptor avidity to recognize tumor-associated antigens and tumor cytolytic activity by CD8+ T cells.

  • GC31675 structure
    GC31675PF-06260933
    CAS: 1811510-56-1
    纯度: >98.00%

    A MAP4K4 inhibitor

  • GC33123 structure
    GC33123GNE 220
    CAS: 1199590-75-4

    GNE-220是一种有效的选择性MAP4K4抑制剂，IC50为7nM。

  • GC34208 structure
    GC34208GNE 220 Hydrochloride
    CAS: 2448286-21-1
    纯度: >98.00%

    GNE220(Hydrochloride)是一种有效的选择性MAP4K4抑制剂，其IC50值为7nM。

  • GC50252 structure
    GC50252PF 06260933 dihydrochloride

    MAP4K4 (HGK) inhibitor; also inhibits MINK and TNIK

  • GC50295 structure
    GC50295TL4-12
    CAS: 1620820-12-3
    纯度: >98.50%

    TL4 12 是一种有效的选择性 GCK（生发中心激酶）抑制剂。

  • GC62514 structure
    GC62514HPK1-IN-3
    CAS: 2739844-34-7
    纯度: >98.50%

    HPK1-IN-3 是一种有效的选择性 ATP 竞争性造血祖细胞激酶 1 (HPK1; MAP4K1) 抑制剂，IC50 为 0.25 nM。HPK1-IN-3 具有 IL-2 细胞效力，在人外周血单核细胞 (PBMC) 中的 EC50 为 108 nM。

  • GC63006 structure
    GC63006HPK1-IN-7
    CAS: 2320462-65-3
    纯度: >99.50%

    HPK1-IN-7 是一种有效的口服活性 HPK1 (造血祖细胞激酶1, MAP4K1) 抑制剂(IC50=2.6 nM)，具有优良的家族和激酶组选择性。HPK1-IN-7 对 IRAK4 (59 nM) 和 GLK (140 nM) 具有选择性。HPK1-IN-7 联合抗 PD1 对 MC38 同基因肿瘤模型显示出强大的疗效。

  • GC63059 structure
    GC63059MAP4K4-IN-3
    CAS: 1811510-58-3
    纯度: >99.00%

    MAP4K4-IN-3 is a potent and selective Mitogen-activated protein kinase 4 (MAP4K4) inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay.

  • GC63317 structure
    GC63317HPK1-IN-8
    CAS: 1214561-09-7

    HPK1-IN-8 是一种变构、非活性构象选择性全长 HPK1 抑制剂。

  • GC63569 structure
    GC63569HPK1-IN-4
    CAS: 2739844-28-9

    HPK1-IN-4 (comp 22) 是 HPK1 (MAPK41) 的抑制剂 (IC50 = 0.061 nM)，用于免疫治疗的研究。

  • GC65298 structure
    GC65298DMX-5804
    CAS: 2306178-56-1
    纯度: >99.00%

    DMX-5804 is a potent, orally active and selective inhibitor of Mitogen-activated protein kinase kinase kinase kinase-4 (MAP4K4) with IC50 of 3 nM for human MAP4K4. DMX-5804 is more potent on human MAP4K4 with pIC50 of 8.55 than MINK1/MAP4K6 and TNIK/MAP4K7 with pIC50 of 8.18 and 7.96, respectively.

  • GC69238 structure
    GC69238HPK1-IN-19
    CAS: 2227609-33-6
    纯度: >98.00%

    KIF18A-IN-1 是一种造血祖细胞激酶 1 HPK1 的抑制剂，详细信息请参考专利文献 WO2018102366A1 中的化合物 I-47。

  • GC69239 structure
    GC69239ZYF0033
    CAS: 2380300-79-6

    ZYF0033 (HPK1-IN-22, compound ZYF0033) 是一种造血祖细胞激酶 1 (HPK1) 抑制剂，基于 MBP 蛋白的磷酸化抑制作用的 IC50 小于 10 nM。ZYF0033 降低 SLP76 (丝氨酸 376) 的磷酸化。ZYF0033 促进抗癌免疫反应。ZYF0033 抑制 4T-1 同基因小鼠模型中的肿瘤生长并导致 DC、NK 细胞和 CD107a+CD8+ T 细胞的肿瘤内浸润增加，但导致 T 细胞、PD-1+CD8+ T 细胞、TIM-3+CD8+ T 细胞和 LAG3+CD8+ T 细胞的浸润减少。

  • GC69240 structure
    GC69240HPK1-IN-32
    CAS: 2766481-17-6
    纯度: >98.00%

    HPK1-IN-32 是一种有效的选择性 HPK1 抑制剂，IC50 为 65 nM。HPK1-IN-32 可用于 HPK1 相关疾病的研究。

  • GC70890 structure
    GC70890HPK1-IN-26
    CAS: 2229042-24-2
    纯度: >98.00%

    HPK1-IN-26是从专利WO2021254118A1化合物1中提取的HPK1和GLK抑制剂。

  • GC73012 structure
    GC73012HPK1-IN-2 dihydrochloride
    CAS: 2375595-72-3
    纯度: >98.00%

    HPK1-IN-2 dihydrochloride是一种强效的口服活性造血祖细胞激酶-1（HPK1）抑制剂（IC50<0.05µΜ），具有抗肿瘤活性。

  • GC73213 structure
    GC73213GNE-6893
    CAS: 2415374-98-8
    纯度: >99.00%

    GNE-6893是一种有效的口服活性HPK1抑制剂。

  • GC73214 structure
    GC73214(3S,4R)-GNE-6893
    CAS: 2415374-97-7
    纯度: >99.00%

    (3S,4R)-GNE-6893是一种强效的口服活性HPK1抑制剂。

  • GC73438 structure
    GC73438HPK1-IN-34
    CAS: 2380300-99-0
    纯度: >95.00%

    HPK1-IN-34（化合物143）是一种造血祖细胞激酶1（HPK1）抑制剂，IC50为<100 nM。