pim3

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.

TBB (NSC-231634)(NSC-231634) is a highly selective, ATP GTP-competitive inhibitor of casein kinase-2 (CK2).

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).

Uzansertib (INCB053914) is a potent ATP-competitive pan-PIM kinase inhibitor. It exhibits exceptional inhibitory activity against PIM1, PIM2, and PIM3 with IC50 values of 0.24 nM, 30 nM, and 0.12 nM, respectively. Furthermore, Uzansertib demonstrates significant anti-proliferative effects against an assorted range of hematologic tumor cell lines.

VS-II-173 is a novel potent Pim1 and Pim3 inhibitor, selectively inducing AML cell death.

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

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.

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).

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, 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).

(1S,3R,5R)-PIM447 (dihydrochloride) is an inhibitor of PIM with IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2, and 0.369 μM for Pim3.

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].

CDK6 PIM1-IN-1 is a balanced, potent dual inhibitor of CDK6 (IC50: 39 nM) and PIM1 (IC50: 88 nM), also showing inhibitory activity on CDK4 (IC50: 3.6 nM). It significantly inhibits the proliferation of acute myeloid leukemia (AML) cells, arrests the cell cycle in G1 phase, induces cell apoptosis, and demonstrates anti-AML activity.

DMAT (Casein kinase II Inhibitor) is a potent and specific inhibitor of CK2(IC50 value of 130 nM).

Dapolsertib (SEL24-B489) is an orally bioavailable and potent PIM and FLT3-ITD inhibitor, inhibiting PIM1, PIM2, and PIM3, decreasing PIM substrate phosphorylation, and inducing dose-dependent apoptosis in leukemia cells.

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.

4'-O-Methylochnaflavone is a biflavonoid compound extracted from the leaves of Ginkgo biloba L., which inhibits lymphocyte proliferation induced by Con A or LPS.

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.

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.

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

AZD-1897 is a highly efficient ATP-competitive pan-PIM inhibitor with anticancer and antileukemic activity, inhibiting PIM1, PIM2, and PIM3, which can be used to study multiple myeloma.

VB1080 (compound 12) is a potent PIM inhibitor with IC50 values of 69.5 µM for PIM1, 4996 µM for PIM2, and 9.88 µM for PIM3. Additionally, VB1080 exhibits cytotoxic properties and possesses anthelmintic activity.

HS38 is a specific and ATP-competitive DAPK inhibitor with Kds of 300 nM, 200 nM, and 280 nM for DAPK1, PIM3, and ZIPK. HS38 can be used in studies about smooth muscle-related disorders.