pim in 1

PIM-IN-1 is a pan-PIM kinase inhibitor with an EC50 of 61 nM in KG-1 and an EC50 of 71 nM in pS6.

PIM-1 CK2-IN-2 (compound 3aA) is an inhibitor of the PIM-1 CK2 enzymes. This compound can induce the mitochondrial apoptosis pathway in CCRF-CEM cells and is utilized in cancer research.

PIM-1 HDAC-IN-1 (compound 4d) is a potent PIM-1 inhibitor with an IC50 of 343.87 nM, and it exhibits strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. Additionally, it induces apoptosis and causes G2 M phase cell cycle arrest in MCF-7 cell lines, specifically inducing pre-G1 apoptosis [1].

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

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

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.

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].

PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor with an IC50 of 0.60 μM and exhibits high cytotoxicity on HCT-116 and MCF-7 cells, with IC50 values of 1.51 μM 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.

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.

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

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 [HS-56].

PIM1-IN-7 (compound 6c) is a potent PIM-1 inhibitor with an IC50 of 0.67 μM, and it also shows notable cytotoxicity against HCT-116 and MCF-7 cells, with IC50 values of 42.9 and 7.68 μM, respectively [1].

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

Compound 5b, designated as Pim-1 2 kinase inhibitor 2, acts as a competitive inhibitor of both PIM-1 and PIM-2 kinases, demonstrating IC50 values of 1.31 μM and 0.67 μM, respectively. This compound exhibits potent in-vitro anticancer activity against various cancer cell lines, including myeloid leukemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2), while showing low cytotoxicity to the normal human lung fibroblast Wi-38 cell line [1].

PIM1-IN-1 is a potent and highly selective inhibitor of PIM1 3 (IC50s: 7 nM for PIM1, 5530 nM for PIM2, and 70 nM for PIM3) with antiproliferative and anti-cancer activity.

PIM1-IN-3 (Compound HL8) is a potent, selective PIM-1 enzyme inhibitor that effectively induces apoptosis in Colo320 cells, demonstrating significant research potential for cancer diseases.

PIM-1 Inhibitor 2 (PIM1-IN-2) is a potent Pim-1 inhibitor with potential anti-cancer activity, used in cancer research.

IBL-302 (AMU302), an orally available dual-signaling inhibitor targeting PIM and PI3K AKT mTOR, is effective against breast cancer and neuroblastoma. It has shown in vivo efficacy in a nude mouse xenograft model by combating trastuzumab resistance. Additionally, IBL-302 augments the effectiveness of widely used cytotoxic chemotherapy drugs such as cisplatin, doxorubicin, and etoposide [1] [2] [3].

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.

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].

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].

PIM-IN-2 (Pim-2) is a potent inhibitor of Pim kinases with an IC50 value of 25 nM, exhibiting antiapoptotic properties that promote cell survival and show elevated expression levels in various human tumors [1].

Protein kinase inhibitor 11 (Compound I-96) is an agent that inhibits the activity of PIM-1, CDK-2, GSK-3, and SRC. It shows potential for research in cancer, autoimmune diseases, and neurodegenerative disorders.