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HS56 (Pim-DAPK3 inhibitor HS56) is a potent, dual Pim/DAPK3 inhibitor with Ki of 72 nM (Pim-3) and 315 nM (DAPK3), shows micromolar potency toward Pim-1 and Pim-2 (Ki=1.5 and 17 uM); displays a high degree of selectivity for DAPKs and Pims against a panel of 468 kinases, with only two off-target interactions TYK2 and GAK; also displays no significant inhibition or activation of nicotinic, adrenergic, or muscarinic receptors at 10 uM; HS56 delayed force onset, decreased contractile force, and reduced LC20 phosphorylation in excised rat caudal arterial VSM tissues, lowers blood pressure in spontaneously hypertensive mice without affecting heart rate.




GDC-0339 is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma.

Blood Cancer





A highly potent and selective inhibitor of pan-Pim with IC50s of 6/18/9 pM for Pim/1/2/3 respectively; induces apoptosis by a decrease in phospho-Bad Ser112 and c-Myc levels and the inhibition of mTORC1 pathway; significantly reduces the tumor burden and prevents tumor-associated bone loss in a murine model of human myeloma.

Blood Cancer

Phase 2 Clinical



1627962-21-3 VS-II-173 is a highly potent Pim1 and Pim3 inhibitor with IC50 of 70 and 20 nM respectively, and a potent and selective inducer of AML cell death (IC50=5.5 uM, Molm-13 cell); acts synergistically with the anthracycline daunorubicin, and additively with a number of other anti-cancer drugs; attenuates phosphorylation of Pim kinase substrates, shows towards cell lines harboring the FLT3-ITD mutation (Molm-13, FLT3-ITD heterozygous and MV4-11 FLT3-ITD homozygous) with EC50 of 2-3 uM; also induces cell death also in AML patient blasts, including blast carrying high-risk FLT3-ITD mutation.

Pim inhibitor 28

Pim inhibitor 28 is a potent, selective inhibitor of Pim1/2 with IC50 of 0.05 nM for both, demonstrates on-target Pim activity in an in vivo pharmacodynamic assay with significant inhibition of BAD phosphorylation in KMS-12-BM multiple myeloma tumors.

pan-PIM inhibitor 17

1681021-52-2 pan-PIM inhibitor 17 is a potent, selective, orally available inhibitor of Pim kinase with IC50 of 0.8, 5.1 and 1.8 nM for Pim1, 2 and 3, respectively; disaplays broad selectivity in an internal panel of 192 kinases, only eight kinases were inhibited above 50% at 1 uM; demonstrates cellular biomarker pS6 inhibition with EC50 of 27 nM, shows tumor growth inhibition in a KG1 tumor-bearing mouse model.


YLT-11 (PLK4 inhibitor YLT11) is a novel potent, selective, ATP-competitive PLK4 inhibitor with IC50 of 22 nM, Kd of 5.2 nM; displays good selectivity over other PIMs and a panel of mitotic kinases, including JNK, TOPK, ERK, and so on; significantly decreases the viability of different subtypes of breast cancer cells with IC50 of 68-120 nM (MDA-MB-231, MDA-MB-468, BT549, and MCF-7 cells), also potently suppresses the DNA replication of cancer cells; significantly suppresses the tumor growth in human breast cancer xenograft models, orally active.

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