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-143898
    PIM1-IN-4
    Inhibitor
    PIM1-IN-4 (Compound 8) is a potent inhibitor of PIM1. PIM1-IN-4 reveals strong inhibition of five other enzymes, i.e., SGK-1, PKA, CaMK-1, GSK3β, and MSK1. PIM1-IN-4 has the potential for the research of cancer diseases.
    PIM1-IN-4
  • HY-15901A
    LGB321 monohydrochloride
    Inhibitor
    LGB321 monohydrochloride is a potent, selective, orally active and ATP competitive inhibitor of all three PIM kinases. LGB321 monohydrochloride inhibits proliferation, mTOR-C1 signaling and phosphorylation of BAD in a number of cell lines derived from diverse hematologic malignancies. LGB321 monohydrochloride can be used for the research of hematologic malignancies.
    LGB321 monohydrochloride
  • HY-RS10554
    Pim3 Mouse Pre-designed siRNA Set A
    Inhibitor

    Pim3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pim3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Pim3 Mouse Pre-designed siRNA Set A
    Pim3 Mouse Pre-designed siRNA Set A
  • HY-174302
    PIM-1/HDAC-IN-2
    Inhibitor
    PIM-1/HDAC-IN-2 is a robust PIM/HDAC inhibitor (IC50 = 0.11 μM in MV4-11cells), which exerts a synergistic antiproliferative effect through a dual mechanism of inhibiting PIM1 kinase and selectively inhibiting HDAC6. PIM-1/HDAC-IN-2 induces cell apoptosis. PIM-1/HDAC-IN-2 remarkably induces the cleavage of PARP, thereby initiating the arrest of the cell cycle in G1 phase and a reduction in S phase. PIM-1/HDAC-IN-2 demonstrates significant anticancer efficacyin the MV4-11 xenograft model without notable toxicity[1].
    PIM-1/HDAC-IN-2
  • HY-150731
    Pim-1 kinase inhibitor 3
    Inhibitor
    Pim-1 kinase inhibitor 3 (Compound H5) is a potent Pim-1 kinase inhibitor with an IC50 of 35.13 nM.
    Pim-1 kinase inhibitor 3
  • HY-132867
    MNK/PIM-IN-1
    Inhibitor
    MNK/PIM-IN-1 represents an innovative dual MNK/PIM inhibitor with a good pharmacokinetic profile.
    MNK/PIM-IN-1
  • HY-RS10553
    PIM3 Human Pre-designed siRNA Set A
    Inhibitor

    PIM3 Human Pre-designed siRNA Set A contains three designed siRNAs for PIM3 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    PIM3 Human Pre-designed siRNA Set A
    PIM3 Human Pre-designed siRNA Set A
  • HY-156470
    Multi-kinase-IN-6
    Inhibitor
    Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that shows good enzyme inhibitory activity against TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. Multi-kinase-IN-6 reveals antiproliferative activity against MCF7, HCT116 and EKVX with IC50 values of 3.36 μM, 1.40 μM and 3.49 μM, respectively. Multi-kinase-IN-6 shows cell cycle arrest at the G1/S phase and G1 phase in MCF7 and HCT116 cells with good apoptotic effect.
    Multi-kinase-IN-6
  • HY-143233
    PIM-1/HDAC-IN-1
    Inhibitor
    PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC50 of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC50 values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase.
    PIM-1/HDAC-IN-1
  • HY-163119
    Pim-1 kinase inhibitor 9
    Inhibitor
    Pim-1 kinase inhibitor 9 (compound 8b) is a selective inhibitor against Pim-1 kinase with IC50 value of 0.24 µM. Pim-1 kinase inhibitor 9 inhibits cell cycle of T47D at S phase. Pim-1 kinase inhibitor 9 reveals antitumor activity.
    Pim-1 kinase inhibitor 9
  • HY-149976
    Pim-1 kinase inhibitor 4
    Inhibitor
    Pim-1 kinase inhibitor 4 (Compound 10f) is a Pim-1 kinase inhibitor (IC50: 17.01 nM). Pim-1 kinase inhibitor 4 also has antioxidant activity and inhibits DPPH. Pim-1 kinase inhibitor 4 induces apoptosis in PC-3 cell, and inhibits PC-3 cell growth with an IC50 of 16 nM. Pim-1 kinase inhibitor 4 can be used for research of prostate cancer.
    Pim-1 kinase inhibitor 4
  • HY-160006
    PIM-IN-2
    PIM-IN-2 (Pim-2) is a Pim kinases inhibitor (IC50 = 25 nM). PIM-IN-2 promotes cell survival, is antiapoptotic, and has exhibited an elevated level of expression in a variety of human tumors.
    PIM-IN-2
  • HY-13287A
    SGI-1776
    Inhibitor
    SGI-1776 is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, Pim-2 and Pim-3, respectively.
    SGI-1776
  • HY-120561
    PC-046
    Inhibitor
    PC-046 is a multi-target inhibitor for tyrosine receptor kinase B (TrkB), IRAK-4 and Pim-1, with IC50 of 13.4 μM, 15.4 μM and 19.1 μM, respectively. PC-046 exhibits cytotoxicity against pancreatic cancer cell BxPC3 with IC50 of 7.5-130 nM. PC-046 induces apoptosis and arrests cell cycle at G2/M phase in BxPC3. PC-046 exhibits antitumor efficacy and exhibits good pharmacokinetic characteristics in mice.
    PC-046
  • HY-15698B
    CRT0066101 trihydrochloride
    Inhibitor
    CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.
    CRT0066101 trihydrochloride
  • HY-163442A
    PIM3-IN-1 hydrochloride
    Inhibitor
    PIM3-IN-1 hydrochloride (Compound 19a) is an inhibitor of (PIM2/3), with the highest inhibition level being against PIM3, having an IC50 value in the nanomolar range. PIM3-IN-1 hydrochloride can be used in cancer research.
    PIM3-IN-1 hydrochloride
  • HY-149996
    Pim-1 kinase inhibitor 6
    Inhibitor
    Pim-1 kinase inhibitor 6 (Compound 4d) is a potent Pim-1 kinase inhibitor with IC50 value of 0.46 μM, and has significant cytotoxic effect on cancer cells.
    Pim-1 kinase inhibitor 6
  • HY-143897
    PIM1-IN-3
    Inhibitor
    PIM1-IN-3 (Compound HL8) is a potent inhibitor of PIM1. PIM1-IN-3 shows selective inhibition for the PIM-1 enzyme. PIM1-IN-3 induces apoptosis efficiently in Colo320 cells. PIM1-IN-3 has the potential for the research of cancer diseases.
    PIM1-IN-3
  • HY-143295
    Pim-1 kinase inhibitor 1
    Inhibitor
    Pim-1 kinase inhibitor 1 is a Pim-1 kinase inhibitor with an IC50 of 0.11 μM for Pim-1 kinase. Pim-1 kinase inhibitor 1 shows anticancer activity to several cancer cell lines by promotes cell apoptosis. Pim-1 kinase inhibitor 1 can be used for the research of cancer.
    Pim-1 kinase inhibitor 1
  • HY-162059
    Pim-1 kinase inhibitor 10
    Inhibitor
    Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation.
    Pim-1 kinase inhibitor 10
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