Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and potential anticancer activity, and inhibits DPPH.Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits the growth of PC-3 cells with an IC50 value of 16 nM. Pim-1 kinase inhibitor 4 promotes apoptosis and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used in prostate cancer research.

TCS-PIM-1-4a (SMI-4a), a Pim inhibitor, blocks mTORC1 activity through activation of AMPK and kills a wide range of both myeloid and lymphoid cell lines (IC50=0.8-40 μM).

Pim-1 kinase inhibitor 8 is a potent Pim-1 kinase inhibitor with anticancer activity and can effectively inhibit cell migration.Pim-1 kinase inhibitor 8 is cytotoxic to MCF-7 and HepG2 cells, and is a candidate compound for breast cancer research.

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

TCS PIM-1 1 (SC 204330)(sc-204330) is a effective and specific ATP-competitive Pim-1 kianse inhibitor (IC50: 50 nM) , exhibits good specific over MEK1/MEK2 and Pim-2(IC50s >20, 000 nM).

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].

(Z)-SMI-4a (TCS PIM-1 4a) is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM.

PIM-1 Inhibitor 2 is an effective Pim-1 kinase inhibitor (Ki = 91 nM).

Pim-1 kinase inhibitor 1 can be used in cancer research, showing anticancer activity against a variety of cancer cell lines by promoting cell apoptosis. Pim-1 kinase inhibitor 1 is an inhibitor of Pim-1 kinase with an IC 50 value of 0.11 μM [1].

Pim-1 kinase inhibitor 5 (Compound 4c), with an IC50 of 0.61 μM, exhibits cytotoxicity against various cancer cell lines, including HepG2, MCF-7, PC3, and HCT-116, with IC50 values ranging from 6.95 to 20.19 μM [1].

Pim-1 kinase inhibitor 2 (Compound 13), a potent inhibitor of Pim-1 kinase, has the potential for cancer research due to its ability to induce apoptosis [1].

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

Pim-1 kinase inhibitor 3 (Compound H5) is a potent inhibitor of Pim-1 kinase, demonstrating an inhibitory concentration (IC50) of 35.13 nM [1].

Pim-1/2 Kinase Inhibitor 1, an orally active inhibitor, impedes the action of Pim kinases by preventing their ability to phosphorylate peptides. It particularly inhibits the phosphorylation of 4E-BP1 and p27 Kip1 by Pim protein kinases. This compound is valuable in cancer research, with a notable application in studying prostate cancer [1].

M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.

Inecalcitol (TX 522) is the growth inhibitor of human breast cancer cells. Inecalcitol is a unique vitamin D3 analog with Kd of 0.53 nM.

K00135 (IMIDAZOPYRIDAZIN 1) is a selective inhibitor of Pim kinases and can be used in studies about gastric cancer and antileukemic therapeutics.

PIM-IN-2 (Pim-2) is a potent inhibitor of Pim kinases, demonstrating an inhibition concentration half-maximal (IC50) value of 25 nM . It exhibits antiapoptotic properties conducive to cell survival and has been found to have increased expression levels across various human tumors [1].

PIM1-IN-6 (compound 5h) is a potent inhibitor of PIM-1 (IC50: 0.60 μM).PIM1-IN-6 has a high cytotoxic effect on HCT-116 and MCF-7 cells with IC50 values of 1.51 and 15.2 μM, respectively.

SGI-1776 (Pim-Kinase Inhibitor IX) has been used in trials studying the treatment of Prostate Cancer, Non-Hodgkins Lymphoma, and Relapsed/Refractory Leukemias.

SMI-16a (PIM1/2 Kinase Inhibitor VI) , a cell-permeable thiazolidinedione compound, acts as an effective, ATP-competitive inhibitor against Pim-1/2 kinases (IC50: 150/20 nM) while exhibiting little or no activity against a panel of 57 other kinases (≤18% inhibition at 5 μM).

Pim1/AKK1-IN-1 (LKB1/AAK1 dual inhibitor) is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AKK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.

CX-6258 hydrochloride hydrate is a potent and selective inhibitor of pan-Pim kinase that acts on Pim-1 (IC50: 5 nM), Pim-2 (IC50: 25 nM) and Pim-3 (IC50: 16 nM).

NDBM, a tumor-specific probe that targets Pim-1 kinase, exhibits heightened fluorescence upon binding and induces cytotoxicity, facilitating both cell screening and killing. It possesses targeted action on lysosomes and a sensitive pH response, enabling the monitoring of intracellular pH variations associated with autophagy and external stimuli [1].

HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor, displaying K i values of 0.26 μM for DAPK3, 0.208 μM for Pim-3, 2.94 μM for Pim-1, and >100 μM for Pim-2. This compound effectively inhibits LC20 phosphorylation and smooth muscle contraction, and reduces blood pressure in spontaneously hypertensive mice, making it a valuable tool for hypertension research.

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

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].

CX-6258 is an orally valid Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor. It has good biological activity and kinase specificity.

Quercetagetin (6-Hydroxyquercetin) (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu. It is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50: 0.34 μM).

FD1024 is a potent PIM inhibitor, displaying inhibitory concentrations (IC50s) of 1.96 nM, 38.9 nM, and 4.17 nM for PIM1, PIM2, and PIM3, respectively. It demonstrates significant antiproliferative effects on several AML cell lines, with IC50 values of 0.16 μM for EOL-1, 0.12 μM for MV-4-11, 1.05 μM for KG-1, and 1.39 μM for MOLM-16. Additionally, FD1024 has shown antitumor efficacy in murine models [1].

TP-3654 is a second-generation Pim kinase inhibitor (Ki values against Pim-1/3: 5/42 nM).

CX-6258 hydrochloride (Pim-Kinase Inhibitor X) is an effective, orally efficacious Pim1/2/3 kinase inhibitor (IC50: 5/25/16 nM).

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.

Cell-permeable peptide inhibitor of Pim-1 kinase, derived from p27Kip1. Inhibits Pim-1 phosphorylation of p27Kip1 and Bad; induces cell cycle arrest (at G1) and apoptosis in DU145 prostate cancer cells. Also inhibits Pim-1-dependent growth of DU145 cells

PIM1-IN-3 (Compound HL8) is a potent inhibitor of PIM1 that selectively inhibits the PIM-1 enzyme and effectively induces apoptosis in Colo320 cells.PIM1-IN-3 has shown research potential for cancer diseases.

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.

Hispidulin, a natural flavone with a broad spectrum of biological activities, is a Pim-1 inhibitor (IC50: 2.71 μM).