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Cat. No. Product Name CAS No. Information
PC-35492

HS56

922050-57-5

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.

PC-45605

PIM-447

1210608-43-7

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

PC-35728

YLT-11

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.
PC-35264

INCB053914

1620012-39-6 INCB053914 (INCB-053914) is a novel potent, and selective ATP-competitive, pan-PIM kinase inhibitor with IC50 of 0.24/30.0/0.12 nM for PIM1/2/3, respectively; INCB053914 is highly selective against a panel of more than 50 kinases (>475-fold selectivity) with exception of RSK2 (IC50=7.1 uM); inhibits cellular proliferation in a panel of cell lines derived from hematologic malignancies including AML, MM, DLBCL, MCL, and T-ALL with GI50 of <100 nM, inhibits proliferation in all MM cell lines with GI5050 of 13.2-230.0 nM; inhibits PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells with IC50 of 4 and 27 nM, also increases PIM2 expression in KG-1a (AML), Pfeiffer, and KMS12-PE cells; in vivo, INCB053914 inhibited Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts.

Solid Tumors

Phase 2 Clinical

PC-63508

SEL24-B489 hydrochloride

SEL24-B489 (SEL24) is a potent, dual PIM and FLT3-ITD inhibitor with Kd of 2/2/3 nM for PIM1/2/3, Kd of 160/16 nM for FLT3-WT/FLT3-ITD, respectively; exhibits significantly broader on-target activity in AML cell lines (MV-4-11 GI50=20 nM) and primary AML blasts than selective FLT3-ITD or PIM inhibitors, decreases viability of AML cells with FLT3-TKD mutations associated with resistance to selective FLT3-ITD inhibitors; inhibits the growth of a broad panel of AML cell lines in xenograft models.

Blood Cancer

Phase 2 Clinical

PC-63507

SEL24-B489

1616359-00-2 SEL24-B489 (SEL24) is a potent, dual PIM and FLT3-ITD inhibitor with Kd of 2/2/3 nM for PIM1/2/3, Kd of 160/16 nM for FLT3-WT/FLT3-ITD, respectively; exhibits significantly broader on-target activity in AML cell lines (MV-4-11 GI50=20 nM) and primary AML blasts than selective FLT3-ITD or PIM inhibitors, decreases viability of AML cells with FLT3-TKD mutations associated with resistance to selective FLT3-ITD inhibitors; inhibits the growth of a broad panel of AML cell lines in xenograft models.

Blood Cancer

Phase 2 Clinical

PC-43464

SGI-1776

1025065-69-3 SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively; exhibits promising selectivity against a panel of >300 kinases, shows inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50=34 nM); reduces cell viability of androgen-independent prostate cancer cell lines with IC50 of 2-4 uM, causes cell cycle arrest and caspase-dependent apoptosis in prostate cancer cells, marginally sensitizes prostate cancer cells to taxane-based therapeutics by inhibiting MDR1 activity and inducing apoptosis; shows efficacy in xenograft model bearing MV-4-11 tumors.

Prostate Cancer

Phase 1 Clinical

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