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  1. JAK/STAT Signaling
  2. Pim

Pim

Pim kinases are a small family of serine/threonine kinases regulating several signaling pathways that are fundamental to cancer development and progression. They were first recognized as pro-viral integration sites for the Moloney Murine Leukemia virus. Pim kinases possess a hinge region which creates a unique binding pocket for ATP. Absence of a regulatory domain means that these proteins are constitutively active once transcribed. Pim kinases are critical downstream effectors of the ABL (ableson), JAK2 (janus kinase 2), and Flt-3 (FMS related tyrosine kinase 1) oncogenes and are required by them to drive tumorigenesis. Recent investigations have established that the Pim kinases function as effective inhibitors of apoptosis and when overexpressed, produce resistance to the mTOR (mammalian target of rapamycin) inhibitor, rapamycin . Overexpression of the PIM kinases has been reported in several hematological and solid tumors (PIM 1), myeloma, lymphoma, leukemia (PIM 2) and adenocarcinomas (PIM 3). As such, the Pim kinases are a very attractive target for pharmacological inhibition in cancer therapy. Novel small molecule inhibitors of the human Pim kinases have been designed and are currently undergoing preclinical evaluation.

Pim 相关产品 (21):

Cat. No.Product NameEffectPurity
  • HY-15604
    AZD1208Inhibitor 99.67%
    AZD1208 是一种新颖,可口服,具有高度选择性的 PIM 抑制剂。
  • HY-19322B
    PIM-447 dihydrochlorideInhibitor 99.67%
    PIM447是泛PIM激酶抑制剂,对PIM1,PIM2,PIM3的Ki 分别为6,18,9 nM。
  • HY-13287
    SGI-1776Inhibitor 99.94%
    SGI-1776 是一种 Pim 抑制剂,抑制 Pim-1,Pim-2 和 Pim-3 的活性,IC50 值分别为 7 nM,363 nM 和 69 nM。
  • HY-10371
    Pim1/AKK1-IN-1Inhibitor 98.10%
    Pim1/AKK1-IN-1 是一种有效的多种酶抑制剂,能够作用于 Pim1/AKK1/MST2/LKB1Kd 值分别为 35 nM/53 nM/75 nM/380 nM。
  • HY-101126
    TP-3654Inhibitor 99.71%
    TP-3654是第二代Pim激酶抑制剂,对Pim-1和Pim-3的Ki值分别为5和42 nM。
  • HY-111552
    PIM1-IN-1Inhibitor
    PIM1-IN-1 是一种有效、高度选择性的 PIM1/3 抑制剂,对 PIM1,PIM2 和 PIM3 的 IC50 值分别为 7,5530 和 70 nM。PIM1-IN-1 抑制 PIM 下游蛋白 BAD 的磷酸化,EC50 值为 262 nM,而对 FLT3 或 hERG 无作用。具有抗增殖、抗肿瘤作用。
  • HY-101783
    GNE-955Inhibitor
    GNE-955是有效的泛Pim激酶抑制剂,Ki分别为18,110,8 nM。
  • HY-N4149
    QuercetagetinInhibitor
    Quercetagetin (6-Hydroxyquercetin) 是从 Citrus unshiu(C. unshiu) 果皮中分离的主要类黄酮。Quercetagetin 是一种中等强度和选择性的,细胞渗透性的 pim-1激酶抑制,IC50 为 0.34 μM。具有抗炎和抗肿瘤活性。
  • HY-N1950
    HispidulinInhibitor 99.33%
    Hispidulin是具有广泛生物活性的天然黄酮。 Hispidulin是Pim-1的抑制剂,IC50值为2.71 μM。
  • HY-18095
    CX-6258Inhibitor 99.13%
    CX-6258是口服活性的Pim 1,2和3激酶抑制剂,IC50为5 nM,25 nM和16 nM。
  • HY-101947
    SMI-16aInhibitor >98.0%
    SMI-16a是选择性的 Pim 激酶抑制剂,对Pim1,Pim2 和 PC3 细胞的IC50值分别为0.15,0.02 和48 μM。
  • HY-18086
    TCS PIM-1 1Inhibitor
    TCS PIM-1 1(sc-204330)是ATP竞争性Pim-1激酶抑制剂,IC50为50nM,比对Pim-2和MEK1/MEK2的抑制性较高。
  • HY-16576
    TCS-PIM-1-4aInhibitor 99.59%
    TCS-PIM-1-4a是Pim抑制剂,能通过AMPK的活化阻断 mTORC1活性,对各种骨髓和淋巴细胞株有杀伤活性,IC50从0.8到40 μM。
  • HY-16976
    GDC-0339Inhibitor 98.49%
    GDC-0339是Pim激酶抑制剂, 作用于BaF3 PIM1时, IC50为43.6 nM。
  • HY-101870B
    INCB053914 phosphateInhibitor 99.91%
    INCB053914 phosphate 是Pim的抑制剂, 来自专利专利WO 2017044730 A1,化合物实例1,IC50值小于35 nM。
  • HY-12830
    M-110Inhibitor
    M-110是Pim激酶抑制剂,抑制前列腺癌细胞系增殖IC50为0.6-0.9uM。
  • HY-15604A
    AZD1208 hydrochlorideInhibitor
    AZD1208 hydrochloride 是一种新颖的,可口服的,具有高度选择性的 PIM 抑制剂。
  • HY-19322
    PIM447Inhibitor
    PIM447是一个新颖的pan-PIM抑制剂。
  • HY-19322C
    (1S,3R,5R)-PIM447 dihydrochlorideInhibitor
    (1S,3R,5R)-PIM447 (dihydrochloride)是PIM的抑制剂,来自专利US 20100056576 A1化合物实例72。对Pim1,Pim2和Pim3的IC50分别为0.095,0.522和0.369 μM.
  • HY-16576A
    (Z)-SMI-4aInhibitor
    (Z)-SMI-4a是ATP竞争性Pim激酶抑制剂,对Pim-1和Pim-2的IC50分别为21nM和100nM,对其它50种激酶几乎无活性。
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