1. JAK/STAT Signaling
  2. Pim

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.

Pim Related Products (17):

Cat. No. Product Name Effect Purity
  • HY-15604
    AZD1208 Inhibitor 99.67%
    AZD1208 is a novel, orally bioavailable, highly selective PIM kinases inhibitor with single nanomolar potency against all three PIM kinases and is currently undergoing Phase I testing and dose escalation studies in AML.
  • HY-19322B
    PIM-447 dihydrochloride Inhibitor 99.67%
    PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.
  • HY-13287
    SGI-1776 Inhibitor 99.70%
    SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM; 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin.
  • HY-10371
    Pim1/AKK1-IN-1 Inhibitor 98.10%
    Pim1/AKK1-IN-1 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.
  • HY-18086
    TCS PIM-1 1 Inhibitor
    TCS PIM-1 1(sc-204330) is a potent and selective ATP-competitive Pim-1 kianse inhibitor with IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2(IC50s >20,000 nM).
  • HY-N1950
    Hispidulin Inhibitor 98.87%
    Hispidulin is a natural flavone with a broad spectrum of biological activities.
  • HY-101126
    TP-3654 Inhibitor 99.71%
    TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
  • HY-101947
    SMI-16a Inhibitor >98.0%
    SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.
  • HY-18095
    CX-6258 Inhibitor 99.13%
    CX-6258 is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.
  • HY-16576
    TCS-PIM-1-4a Inhibitor 99.83%
    TCS-PIM-1-4a is a Pim inhibitor that blocks mTORC1 activity via activation of AMPK; kills a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM).
  • HY-12830
    M-110 Inhibitor
    M-110 is a novel and highly selective inhibitor of PIM kinases; inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 uM, with no activity on normal human peripheral blood mononuclear cells up to 40 uM.
  • HY-16976
    GDC-0339 Inhibitor
    GDC-0339 is a Pim kinase inhibitor with IC50 of 43.6 nM for BaF3 PIM1.
  • HY-19322C
    (1S,3R,5R)-PIM447 dihydrochloride Inhibitor
    (1S,3R,5R)-PIM447 (dihydrochloride) an PIM inhibitor extracted from patent US 20100056576 A1, compound example 72, has IC50 values of 0.095 μM for Pim1, 0.522 μM for Pim2 and 0.369 μM for Pim3.
  • HY-16576A
    (Z)-SMI-4a Inhibitor
    (Z)-SMI-4a is a selective ATP-competitive Pim-1 kinase inhibitor with an IC50 of 21 nM for Pim-1 compared to an IC50 of 100 nM for Pim-2 and with little or no activity against a panel of 50 other kinases tested.
  • HY-19322
    PIM447 Inhibitor
    PIM447 is novel pan-PIM kinase inhibitor, including Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase.
  • HY-18095A
    CX-6258 hydrochloride hydrate Inhibitor
    CX-6258 hydrochloride hydrate is a potent, orally efficacious Pim 1/2/3 kinase(IC50=5 nM/25 nM/16 nM) inhibitor with excellent biochemical potency and kinase selectivity.
  • HY-101870B
    PIM inhibitor 1 phosphate Inhibitor 98.33%
    PAK4-IN-1 is an inhibitor of Pim extracted from patent WO 2017044730 A1, compound 1; has an IC50 of less than 35 nM.