1. Signaling Pathways
  2. JAK/STAT Signaling
  3. Pim

Pim

Pim kinases

The PIM kinase, also known as serine/threonine kinase plays an important role in cancer biology and is found in three different isoforms namely PIM-1, PIM-2, and PIM-3. Pim kinases are mainly responsible for cell cycle regulation, antiapoptotic activity and the homing and migration of receptor tyrosine kinases mediated via the JAK/STAT pathway.

Pim kinases are over-expressed in various types of tumors and regulate the activation of signaling pathways that are important for tumor cell proliferation, survival and expression of drug efflux proteins. This makes Pim kinases attractive targets for the development of anti-cancer chemotherapeutic drugs.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18095A
    CX-6258 hydrochloride hydrate
    Inhibitor 99.23%
    CX-6258 hydrochloride hydrate is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
    CX-6258 hydrochloride hydrate
  • HY-18086
    TCS PIM-1 1
    Inhibitor 98.01%
    TCS PIM-1 1 (SC 204330) is a potent, selective and ATP-competitive Pim-1 kianse inhibitor with an IC50 of 50 nM, displays good selectivity over Pim-2 and MEK1/MEK2 (IC50s >20000 nM).
    TCS PIM-1 1
  • HY-18095B
    CX-6258 hydrochloride
    Inhibitor 99.03%
    CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively.
    CX-6258 hydrochloride
  • HY-15698
    CRT0066101
    Inhibitor
    CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.
    CRT0066101
  • HY-111552
    PIM1-IN-1
    Inhibitor 99.83%
    PIM1-IN-1 is a potent and highly selective PIM1/3 inhibitor, with IC50s of 7, 5530 and 70 nM for PIM1, PIM2, and PIM3, respectively, inhibits the phosphorylation of BAD, a downstream target of PIM, with an EC50 of 262 nM. PIM1-IN-1 shows no obvious effect on FLT3 or hERG binding. Antiproliferative and anti-cancer activity.
    PIM1-IN-1
  • HY-122665
    HTH-01-091
    Inhibitor 98.64%
    HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research.
    HTH-01-091
  • HY-19322C
    (1S,3R,5R)-PIM447 dihydrochloride
    Inhibitor 99.81%
    (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.
    (1S,3R,5R)-PIM447 dihydrochloride
  • HY-15604A
    AZD1208 hydrochloride
    Inhibitor
    AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
    AZD1208 hydrochloride
  • HY-108605
    PIM1-IN-2
    Inhibitor ≥99.0%
    PIM1-IN-2 is a potent and ATP competitive Pim-1 inhibitor with a Ki of 91 nM. PIM1-IN-2 targets the ATP-binding kinase hinge region not by forming classical hydrogen bonds.
    PIM1-IN-2
  • HY-129163
    HJ-PI01
    Inhibitor 99.72%
    HJ-PI01 (10-Acetylphenoxazine) is an orally active Pim-2 inhibitor. HJ-PI01 induces apoptosis and autophagic cell death of cancer cells. HJ-PI01 inhibits tumor growth in MDA-MB-231 xenograft mice. HJ-PI01 can be used for cancer research.
    HJ-PI01
  • HY-157169
    IBL-302
    Inhibitor 98.21%
    IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629).
    IBL-302
  • HY-122665A
    HTH-01-091 TFA
    Inhibitor 99.48%
    HTH-01-091 TFA is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 TFA also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 TFA can be uesd for breast cancer research.
    HTH-01-091 TFA
  • HY-101783
    GNE-955
    Inhibitor
    GNE-955 is a potent and orally active pan Pim kinase inhibitor with Kis of 0.018, 0.11, 0.08 nM for Pim1, Pim2, Pim3, respectively.
    GNE-955
  • HY-101870
    Uzansertib
    Inhibitor
    Uzansertib (INCB053914) is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC50s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
    Uzansertib
  • HY-123983
    HS56
    Inhibitor
    HS56 is an ATP-competitive dual Pim/DAPK3 inhibitor with Ki values of 0.26, 0.208, 2.94, and >100 μM for DAPK3, Pim-3, Pim-1, and Pim-2, respectively. HS56 inhibits LC20 phosphorylation and smooth muscle contraction. HS56 decreases blood pressure in spontaneously hypertensive mice. HS56 can be used in research of hypertension.
    HS56
  • HY-147785
    Pim-1 kinase inhibitor 2
    Inhibitor
    Pim-1 kinase inhibitor 2 (Compound 13) is a potent inhibitor of Pim-1 kinase. Pim-1 kinase inhibitor 2 induces apoptosis. Pim-1 kinase inhibitor 2 has the potential for the research of cancer diseases.
    Pim-1 kinase inhibitor 2
  • HY-P1404
    R8-T198wt
    Inhibitor
    R8-T198wt is a cell-permeable carboxyl-terminal p27Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase.
    R8-T198wt
  • HY-155717
    NDBM
    NDBM is a probe and binds to tumor-specific Pim-1 kinase, releases strong fluorescence, and produces cytotoxicity, thus achieving cell screening and killing effects. NDBM can specifically target lysosomes and sensitively respond to pH. NDBM can be used to track the pH changes in the intracellular environment under conditions of autophagy and external stimulation.
    NDBM
  • HY-162006
    Pim-1 kinase inhibitor 8
    Inhibitor 99.90%
    Pim-1 kinase inhibitor 8 (compound 12) is a potent inhibitor of Pim-1 kinase with an IC50 of 14.3 nM. Pim-1 kinase inhibitor 8 has potent cytotoxicity against MCF-7 and HepG2 cells with IC50s of 0.5 and 5.27 μM, respectively. Pim-1 kinase inhibitor 8 can used in study breast cancer.
    Pim-1 kinase inhibitor 8
  • HY-142656
    PIM-IN-1
    Inhibitor
    PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC50 = 61 nM; pS6, EC50 = 71 nM).
    PIM-IN-1
Cat. No. Product Name / Synonyms Application Reactivity

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