Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12474 |
PIM1-IN-1
|
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
PIM1-IN-1 is a potent and highly selective inhibitor of PIM1/3(IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively),with Antiproliferative and anti-cancer activity. | |||
T5093 |
Pim1/AKK1-IN-1
LKB1/AAK1 dual inhibitor,MDK-2275 |
Pim; Hippo pathway | Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells |
Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) 是多种酶抑制剂,能够作用于Pim1、AKK1、MST2 和 LKB1,Kd 值分别为 35、53、75 和 380 nM,还抑制 MPSK1 和 TNIK。 | |||
T10828 |
CK2/PIM1-IN-1
|
Others | Others |
CK2/PIM1-IN-1 is an inhibitor of CK2 and PIM1 (IC50s: 3.787 μM and 4.327 μM). It is developed for the research of proliferative disorders such as cancer, as well as other kinase-associated conditions. | |||
T63071 |
CDK6/PIM1-IN-1
|
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CDK6/PIM1-IN-1 是一种平衡的、有效的、双重 CDK6 (IC50: 39 nM) 和 PIM1 (IC50: 88 nM) 抑制剂。CDK6/PIM1-IN-1 对 CDK4 表现出抑制作用,其 IC50 值为 3.6 nM。CDK6/PIM1-IN-1 能够明显抑制急性髓系白血病 (AML) 细胞增殖,将细胞周期阻滞在 G1 期并诱导细胞凋亡。CDK6/PIM1-IN-1 表现出抗 AML 活性。 | |||
T10827 |
CK2/ERK8-IN-1
TMCB |
Apoptosis; ERK; Casein Kinase; Pim; DYRK | Apoptosis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors |
CK2/ERK8-IN-1 (TMCB) 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 也与 PIM1,HIPK2 和 DYRK1A 结合,Ki 值分别为 8.65 µM,15.25 µM 和 11.9 µM。 | |||
T73247 | PIM1-IN-4 | Pim | Chromatin/Epigenetic; JAK/STAT signaling |
PIM1-IN-4(Compound 8)为PIM1高效抑制剂,对SGK-1、PKA、CaMK-1、GSK3β及MSK1五种酶亦展现出显著抑制效应,表现出其在癌症疾病研究中的应用潜力。 | |||
T63720 | PIM1-IN-3 | ||
PIM1-IN-3 (Compound HL8) 是一种 PIM1 的有效抑制剂,能够选择性抑制 PIM-1 酶,可有效的诱导 Colo320 细胞凋亡。PIM1-IN-3 对癌症疾病表现出研究潜力。 | |||
T62188 |
PIM1-IN-6
|
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PIM1-IN-6 (compound 5h) 是一种 PIM-1 的有效抑制剂 (IC50: 0.60 μM)。PIM1-IN-6 对 HCT-116 和 MCF-7 细胞具有较高的细胞毒作用,他们的 IC50 值分别为 1.51 和 15.2 μM。 | |||
T61700 | PIM1-IN-7 | ||
PIM1-IN-7 (compound 6c) is a powerful inhibitor of PIM-1, effectively suppressing its activity with an IC50 of 0.67 μM. This compound also exhibits significant cytotoxicity against HCT-116 and MCF-7 cells, as demonstrated by their respective IC50 values of 42.9 and 7.68 μM [1]. | |||
T79456 |
FD1024
|
Pim | Chromatin/Epigenetic; JAK/STAT signaling |
FD1024是一种PIM抑制剂,对PIM1、PIM2和PIM3的IC50s分别为1.96、38.9及4.17 nM。用于急性髓系白血病研究的FD1024,对AML细胞系显示出显著的抗增殖效果,其对EOL-1、MV-4-11、KG-1和MOLM-16细胞的抑制浓度(IC50s)分别为0.16 μM、0.12 μM、1.05 μM和1.39 μM。此外,FD1024在小鼠模型中也表现出抗肿瘤活性。 | |||
T81740 | Multi-kinase-IN-6 | Trk receptor | Tyrosine Kinase/Adaptors |
Multi-kinase-IN-6 (compound 10e) 是一种效能极高的多激酶抑制剂,具有对 TrkA、ALK2、c-KIT、EGFR、PIM1、CK2α、CHK1 和 CDK2 等多种酶的显著抑制作用。在 MCF7、HCT116 和 EKVX 癌细胞系上,其抗增殖活性突出,IC50 值分别达到 3.36 μM、1.40 μM 与 3.49 μM。此外,Multi-kinase-IN-6 能引起 MCF7 与 HCT116 细胞的细胞周期在 G1/S 期及 G1 期停滞,并有效诱导凋亡。 |