pim 2

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].

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

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

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].

HJ-PI01 (HJ-PI01) is a Pim-2 inhibitor. HJ-PI01 (HJ-PI01) induces apoptosis and autophagic cell death in triple-negative human breast cancer.

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.

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

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).

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

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.

Uzansertib phosphate (INCB053914 phosphate) is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively).

GDC-0339 is discovered as a potential treatment of multiple myeloma. GDC-0339 is an orally bioavailable and well-tolerated inhibitor of pan-Pim kinase (Kis: 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively).

GNE-955 is a potent and orally active inhibitor of pan Pim kinase, with inhibition constants (Kis) of 0.018 nM, 0.11 nM, and 0.08 nM for Pim1, Pim2, and Pim3, respectively.

AZD1208 is a novel, orally bioavailable, highly selective PIM kinase inhibitor with single nanomolar potency against all three PIM kinases.

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).

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

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

PIM-35, an indole derivative with properties similar to antidepressants, exhibits weaker norepinephrine uptake inhibition compared to standard compounds. Prolonged use of PIM-35 does not affect the quantity or affinity of alpha 2, beta 1-, and beta 2-adrenergic receptors. Additionally, PIM-35 influences the serotonin system, resembling antidepressant compounds like paroxetine and clomipramine.

Protein Kinase Inhibitor 12 (compound 1-91) is a triazole derivative and protein kinase inhibitor, particularly effective against PIM-1, CDK-2, GSK-3, and SRC mammalian protein kinases, and can be used to study diseases related to protein kinases.

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.

Protein kinase inhibitor 13 (Compound I-90) functions as a kinase inhibitor, specifically targeting kinases such as PIM-1, CDK-2, GSK-3, and SRC.