pim-in-1

PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC 50 = 61 nM; pS6, EC 50 = 71 nM).

MNK/PIM-IN-1 is a novel dual inhibitor targeting both MNK and PIM pathways, characterized by its favorable pharmacokinetic profile.

Pim-IN-14j is a potent, highly selective, and orally bioavailable inhibitor of PIM-1 kinases.

MK1496 is a n orally bioavailable Polo-like kinase 1 (Plk1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor MK1496 selectively inhibits Plk1, inducing selective G2 M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

K00135 (IMIDAZOPYRIDAZIN 1) 是 Pim 激酶的选择性抑制剂，可用于胃癌和抗白血病治疗的研究。

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。

Pim-1 2 kinase inhibitor 1 是一种具有口服活性的 Pim-1 2 激酶抑制剂。Pim-1 2 kinase inhibitor 1 能阻断 Pim 激酶磷酸化肽的能力，并且抑制4E-BP1和p27Kip1的Pim 蛋白激酶定向磷酸化。Pim-1 2 kinase inhibitor 1 可用于癌症，尤其是前列腺癌的研究。

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.

PIM-1 CK2-IN-2 (compound 3aA) 作为一种PIM-1 CK2抑制剂，在CCRF-CEM细胞中可激活线粒体凋亡途径，常用于癌症研究。

Protein kinase inhibitor 11 (Compound I-96) 是一种蛋白激酶抑制剂，能够抑制PIM-1、CDK-2、GSK-3和SRC的活性。此化合物被期望应用于癌症、免疫性疾病和神经退行性疾病的研究。

PIM-1 Inhibitor 2 (PIM1-IN-2) 是一种高效性 Pim-1 抑制剂，具有潜在的抗癌活性，可用于研究癌症。

SGI-1776 (Pim-Kinase Inhibitor IX) 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。

Pim-1 kinase inhibitor 1 可用于癌症领域研究， 通过促进细胞凋亡对多种癌细胞系表现出抗癌活性。Pim-1 kinase inhibitor 1 是一种Pim-1 激酶抑制剂 (IC50 = 0.11 μM)。

PIM-1 HDAC-IN-1 (compound 4d) is a potent inhibitor of PIM-1, with an IC 50 of 343.87 nM. It also exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC 50 values of 63.65 and 62.39 nM, respectively. Furthermore, PIM-1 HDAC-IN-1 demonstrates apoptosis-inducing potential in MCF-7 cell lines, specifically inducing pre-G1 apoptosis and causing cell cycle arrest at the G2 M phase [1].

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].

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。

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。

HS56 是一种 ATP 竞争性 Pim DAPK3双重抑制剂，对 DAPK3、Pim-3、Pim-1和 Pim-2 的 Ki 值分别为 0.26、0.208、2.94 和 ＞100 μM。 HS56 抑制 LC20 磷酸化和平滑肌收缩。HS56 降低自发性高血压小鼠的血压。HS56可用于高血压研究。

Pim-1 kinase inhibitor 4 是一种高效的 Pim-1 激酶 抑制剂，IC50 值为 17.01 nM。Pim-1 kinase inhibitor 4 还具有抗氧化活性和潜在的抗癌活性，对 DPPH 有抑制作用。Pim-1 kinase inhibitor 4 促进 PC-3 细胞凋亡 (apoptosis)，对 PC-3 细胞生长有抑制作用，IC50 为 16 nM。Pim-1 kinase inhibitor 4 可用于研究前列腺癌。

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。

PIM-IN-2是Pim激酶抑制剂，具有25 nM 的半抑制浓度(IC50)。它能增强细胞存活、防止凋亡，并在多种人类肿瘤中高表达。

QLT0267 is an inhibitor targeting integrin-linked kinase (ILK; IC50= 26 nM), showing over 10-fold selectivity against cyclin-dependent kinases 1, 2, and 5 (Cdk1, Cdk2, and Cdk5), and over 1,000-fold selectivity against C-terminal Src kinase (CSK), DNA-PK, Pim-1, Akt, PKC, and casein kinase 2 (CK2) at a concentration of 10 mg/ml. This compound effectively inhibits the proliferation of NPA187 papillary thyroid cancer cells with an IC50 of approximately 3 µM and induces apoptosis in NPA187, DRO, and K4 cancer cell lines. In vivo studies reveal that QLT0267, administered at 100 mg/kg, significantly reduces tumor growth in a DRO mouse xenograft model and diminishes both tumor volume and intratumoral vascularization in a U87MG glioblastoma mouse xenograft model, showcasing its potential for therapeutic applications in cancer treatment.

IBL-302 (AMU302) 是一种口服有效的PIM和PI3K AKT mTOR双信号抑制剂，具有抗乳腺癌和成神经细胞瘤的活性。在裸鼠异种移植模型中，IBL-302 显示出体内效力，并能抑制曲妥珠单抗的耐药性问题。此外，IBL-302 还能增强顺铂、阿霉素和依托泊苷等常见细胞毒性化疗药物的效果。

Pim-1 2 kinase inhibitor 2 (compound 5b) 作为一种PIM-1和PIM-2激酶的竞争性抑制剂，其IC50值分别为1.31 μM和0.67 μM。该化合物在正常的人类肺成纤维细胞系Wi-38中表现出较低的细胞毒性，并且在体外对多种癌细胞系如骨髓性白血病(NFS-60)、肝癌(HepG-2)、前列腺癌(PC-3)和结肠癌(Caco-2)显示出有效的抗癌活性。