Welcome to Raystarbio!Focus On Forefront Bioactive Compounds.
Find Your Distributors

Select Your Country or Region

$ USD

You are here:Home-Inhibitors & Agonists-JAK/STAT Signaling-Pim

Request The Product List ofPim Pim

Pim kinases are a small family of serine/threonine kinases regulating several signaling pathways that are fundamental to cancer development and progression. They were first recognized as pro-viral integration sites for the Moloney Murine Leukemia virus. Pim kinases possess a hinge region which creates a unique binding pocket for ATP. Absence of a regulatory domain means that these proteins are constitutively active once transcribed. Pim kinases are critical downstream effectors of the ABL (ableson), JAK2 (janus kinase 2), and Flt-3 (FMS related tyrosine kinase 1) oncogenes and are required by them to drive tumorigenesis. Recent investigations have established that the Pim kinases function as effective inhibitors of apoptosis and when overexpressed, produce resistance to the mTOR (mammalian target of rapamycin) inhibitor, rapamycin . Overexpression of the PIM kinases has been reported in several hematological and solid tumors (PIM 1), myeloma, lymphoma, leukemia (PIM 2) and adenocarcinomas (PIM 3). As such, the Pim kinases are a very attractive target for pharmacological inhibition in cancer therapy. Novel small molecule inhibitors of the human Pim kinases have been designed and are currently undergoing preclinical evaluation.

Cat. No. Product Name CAS No. Information
GY02867

PIM-447 dihydrochloride

1808011-22-4

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.

GY02541

GDC-0339

1428569-85-0

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

GY02487

M-110

1395048-49-3

M-110 is a potent, selective inhibitor of PIM kinase family with preference for PIM-3 with IC50 of 0.047, 2.5 and 2.5 uM for PIM3, PIM1 and PIM2, respectively; dispplays excellent selectivity in a panel of 261 kinases; inhibits the growth of DU-145 cells with IC50 of 0.9 uM, significantly reduces pSTAT3(Tyr705) expression without affecting the expression of STAT3, also attenuates the IL-6-induced increase in pSTAT3(Tyr705), shows no effect on phosphorylation of STAT5 on Tyr694 in 22Rv1 cells.

GY02437

TP-3654

1361951-15-6

A potent, selective, orally active second-generation PIM inhibitor with Ki of 5, 42 and 239 nM for Pim1, 2 and 3, respectively; exhibits submicromolar activity in UM-UC-3 bladder cancer cell line; displays favorabl hERG and CYP450 inhibition profiles compared with SGI-1776, reduces tumor growth in vivo xenografts.

GY02419

CX-6258 hydrochloride hydrate

1353858-99-7

A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively; exhibits in vitro synergy with chemotherapeutics and robust in vivo efficacy in driven tumor models; also decreases steady state levels and half-life of NKX3.1 protein but not mRNA in prostate cancer cells.

GY10144

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.

GY10359

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.

GY10396

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.

GY10445

VS-II-173

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.

GY02244

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.

Request The Product List

* Indicates a Required FieldYour information is safe with us.

  • *Product List:
  • *Applicant name:
  • *Email address:
  • *Organization name:
  • *Country:
  • Additional Information:
© Copyright 2020 RayStarBio. All Rights Reserved. Products are only for research use