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

Pim

Pim kinases

Pim

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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
  • HY-15604
    AZD1208
    		Inhibitor 99.71%
    AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.
  • HY-N1950
    Hispidulin
    		Inhibitor 99.66%
    Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.
  • HY-101126
    TP-3654
    		Inhibitor 99.91%
    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-19322B
    PIM-447 dihydrochloride
    		Inhibitor 99.27%
    PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis.
  • HY-10371
    Pim1/AKK1-IN-1
    		Inhibitor 98.20%
    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-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.
  • HY-149995
    Pim-1 kinase inhibitor 5
    		Inhibitor
    Pim-1 kinase inhibitor 5 (Compound 4c) is a Pim-1 kinase inhibitor (IC50: 0.61 μM). Pim-1 kinase inhibitor 5 shows cytotoxicity against cancer cells, with IC50s of 6.95-20.19 μM for HepG2, MCF-7, PC3, and HCT-116 cells.
  • HY-155529
    FD1024
    		Inhibitor
    FD1024 is PIM inhibitor (IC50s: 1.96, 38.9, 4.17 nM for PIM1, 2, 3). FD1024 can be used for research of acute myeloid leukemia. FD1024 has strong antiproliferative activity against the tested AML cell lines, with 0.16 μM, 0.12 μM, 1.05 μM, 1.39μM for EOL-1, MV-4-11, KG-1, MOLM-16 cells. FD1024 also has antitumor efficacy in mice.
  • HY-13287
    SGI-1776 free base
    		Inhibitor 99.23%
    SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.
  • HY-18095
    CX-6258
    		Inhibitor 98.71%
    CX-6258 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.
  • HY-N4149
    Quercetagetin
    		Inhibitor 99.74%
    Quercetagetin (6-Hydroxyquercetin) is a flavonoid. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM). Anti-inflammatory and anticancer properties.
  • 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-101870B
    Uzansertib phosphate
    		Inhibitor 99.39%
    Uzansertib (INCB053914) phosphate 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 phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.
  • HY-16976
    GDC-0339
    		Inhibitor 99.77%
    GDC-0339 is a potent, orally bioavailable and well tolerated pan-Pim kinase inhibitor, with Kis of 0.03 nM, 0.1 nM and 0.02 nM for Pim1, Pim2 and Pim3, respectively. GDC-0339 is discovered as a potential treatment of multiple myeloma.
  • HY-18095A
    CX-6258 hydrochloride hydrate
    		Inhibitor 98.61%
    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.
  • 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).
  • HY-135906
    CK2/ERK8-IN-1
    		Inhibitor ≥99.0%
    CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 (MAPK15, ERK7) inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy.
  • HY-18095B
    CX-6258 hydrochloride
    		Inhibitor 99.28%
    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.
  • HY-120758
    SEL24-B489
    		Inhibitor 98.58%
    SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively.
  • HY-16576A
    SMI-4a
    		Inhibitor 99.63%
    SMI-4a (TCS-PIM-1-4a) is a poten, selective, cell-permeable and ATP-competitive Pim-1 inhibitor with an IC50 of 24 μM and a Ki of 0.6 μM. SMI-4a also inhibits Pim-2 (IC50 of 100 μM), and does not significantly inhibit the other serine/threonine- or tyrosine-kinases. SMI-4a has anticancer activity.
Cat. No. Product Name / Synonyms Application Reactivity