Pim

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-447 dihydrochloride is an orally available and selective inhibitor of pan-PIM kinase(Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively).

PIM1-IN-1 is a potent and highly selective PIM kinase inhibitor with strong preference for PIM1 and PIM3 over PIM2, effectively inhibiting BAD phosphorylation without detectable effects on FLT3 or hERG binding, and exhibiting antiproliferative and anticancer activity suitable for mechanistic studies of PIM-driven oncogenic signaling.

PIM447 (LGH447) is an oral, selective pan-PIM kinase inhibitor with antitumor and bone-protective effects. It inhibits PIM1, PIM2, and PIM3, induces apoptosis, and decreases the viability, proliferation, and motility of HuH6 and COA67 cells. PIM447 suppresses tumorigenesis in hepatocellular carcinoma and can be used in the study of multiple myeloma.

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

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

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

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.

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.

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).

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor (IC50: 10.5 nM) that also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. It can be used to study breast cancer.

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

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).

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.

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

(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).

TP-3654, 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).

HS94 (DAPK3 inhibitor HS94) is a selective and potent DAPK3 inhibitor with a Ki value of 126 nM for Pim kinase inhibition and can be used to study hypertension.

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).

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