1. Signaling Pathways
  2. JAK/STAT Signaling
  3. Pim

Pim (Pim激酶)

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 (12):

Cat. No. Product Name Effect Purity
  • HY-15604
    AZD1208 Inhibitor 99.90%
    AZD1208 是一种有效的,具有口服活性的,具有高度选择性的 PIM 抑制剂。
  • HY-19322B
    PIM-447 dihydrochloride Inhibitor 99.33%
    PIM447 dihydrochloride (LGH447 dihydrochloride) 是一种有效的、口服的、选择性的泛 PIM 激酶抑制剂,对 PIM1、PIM2 和 PIM3 的 Ki 值分别为 6、18 和 9 pM。PIM447 dihydrochloride 具有双重抗肿瘤和骨保护作用。PIM447 dihydrochloride 诱导细胞凋亡。
  • HY-10371
    Pim1/AKK1-IN-1 Inhibitor 98.12%
    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-N1950
    Hispidulin Inhibitor 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-18086
    TCS PIM-1 1 Inhibitor 98.03%
    TCS PIM-1 1 (SC 204330) 是一种有效的,具有选择性和 ATP 竞争性的 Pim-1 激酶抑制剂,IC50 为 50 nM,对 Pim-2 和 MEK1/MEK2 表现出良好的选择性 (IC50 >20000 nM)。
  • HY-18095B
    CX-6258 hydrochloride Inhibitor
    CX-6258 hydrochloride是一种强效的、激酶选择性的 pan-Pim 激酶抑制剂,对 Pim-1, Pim-2 和 Pim-3 作用的 IC50 值分别为 5 nM、25 nM 和 16 nM。
  • HY-12830
    M-110 Inhibitor 98.78%
    M-110 是一种高选择性的,ATP 竞争性的 PIM 激酶抑制剂,M-110 对 PIM-3 抑制作用最好,IC50=47 nM。M-110 抑制 PIM-1 和 PIM-2 的IC50 为 2.5 μM。M-110 抑制前列腺癌细胞的增殖,IC50 为 0.6-0.9 μM。
  • HY-N4149
    Quercetagetin Inhibitor 99.24%
    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-16576
    TCS-PIM-1-4a Inhibitor 99.90%
    TCS-PIM-1-4a (SMI-4a) 是一种泛-Pim 激酶抑制剂,可通过激活 AMPK 来阻断 mTORC1 的活性。TCS-PIM-1-4a 可杀死多种髓样和淋巴样细胞系 (IC50 值为 0.8 μM 至 40 μM)。
  • HY-101947
    SMI-16a Inhibitor 99.70%
    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-135906
    CK2/ERK8-IN-1 Inhibitor >99.0%
    CK2/ERK8-IN-1 是一种酪蛋白激酶 2 (CK2) (Ki 为 0.25 µM) 和 ERK8 (MAPK15, ERK7) 的双重抑制剂,IC50 均为 0.50 μM。CK2/ERK8-IN-1 还与 PIM1HIPK2DYRK1A 结合,Ki 值分别为 8.65 µM,15.25 µM 和 11.9 µM。CK2/ERK8-IN-1 具有促凋亡 (pro-apoptotic) 作用。
  • HY-19322C
    (1S,3R,5R)-PIM447 dihydrochloride Inhibitor 98.13%
    (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。
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