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

Pim

Pim kinases

Pim

Related Products

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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.

Pim Isoform Specific Products:

Pim Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-15604
    AZD1208
    		Inhibitor 99.73%
    AZD1208 is an orally bioavailable, highly selective PIM kinases inhibitor.
    AZD1208
  • HY-N1950
    Hispidulin
    		Inhibitor 99.74%
    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.
    Hispidulin
  • HY-15698A
    CRT0066101 dihydrochloride
    		Inhibitor 99.92%
    CRT0066101 dihydrochloride 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 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects.
    CRT0066101 dihydrochloride
  • HY-101126
    TP-3654
    		Inhibitor 99.96%
    TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.
    TP-3654
  • HY-10371
    Pim1/AKK1-IN-1
    		Inhibitor 98.40%
    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.
    Pim1/AKK1-IN-1
  • HY-115590
    JP-11646
    		Inhibitor 98.74%
    JP-11646 is a pan-PIM inhibitor with increased potency against PIM2 (IC50 = 0.5 nM). JP11646 is freely reversible and ATP non-competitive. JP-11646 results in a decrease of PIM1, 2, and 3 mRNA. JP-11646 can effectively inhibit cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC). JP-11646 can cause a decrease in p-4EBP-1 protein, increasing the cleavage of caspases while decreasing caspase-3. JP-11646 induces apoptosis or necroptosis in cells. JP-11646 leads to reductions in MYC paralogs. JP-11646 can be used for the study of SCLC, LCNEC, human acute leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC).
    JP-11646
  • HY-179538
    CSH-4044
    		Inhibitor
    CSH-4044 can be isolated from fermented wheat germ extract. CSH-4044 is a unique benzothiazole compound. CSH-4044 can inhibit PIM3-driven BAD phosphorylation in pancreatic cancer cell lines as well as reducing DYRK1A-induced Tau phosphorylation in neuronal cells.
    CSH-4044
  • HY-122670
    VS-II-173
    		Inhibitor
    VS-II-173 is a pan-Pim kinase inhibitor with IC50 values ​​of 0.07 μM and 0.02 μM for Pim1 and Pim3, respectively, and a residual activity of 46% for Pim2 at 1 μM. VS-II-173 also inhibits kinases such as HIPK2, PRK2, RSK1, DYRK1a and AMPKα1, selectively inhibiting acute myeloid leukemia (AML) cells with significantly lower toxicity to non-malignant cells (EC50 > 30 μM). VS-II-173 weakens the phosphorylation of substrates such as Stat5 (Y694), MDM2 (S166), Bad (S112), and 4E-BP1 (T37/46) by inhibiting Pim kinase-mediated signaling pathways, blocking pro-survival signals in AML cells and inducing apoptosis. VS-II-173 synergistically enhances anti-AML activity when combined with Daunorubicin (HY-13062A). VS-II-173 can be used in AML research, especially for AML with FLT3-ITD mutations and NPM1 mutations .
    VS-II-173
  • HY-13287
    SGI-1776 free base
    		Inhibitor 99.96%
    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.
    SGI-1776 free base
  • HY-15698
    CRT0066101
    		Inhibitor 99.88%
    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-16576A
    SMI-4a
    		Inhibitor 99.85%
    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.
    SMI-4a
  • HY-19322
    PIM447
    		Inhibitor 99.52%
    PIM447 (LGH447) 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 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis.
    PIM447
  • HY-171579
    RS47
    		Inhibitor 98.0%
    RS47 is a selective RelB inhibitor with a Kd value of 1.1 μM. RS47 also acts as an inhibitor of HCV replication. RS47 can block the non-canonical NF-κB signaling pathway without affecting the canonical pathway. RS47 exerts anti-tumor effects of inhibiting proliferation and promoting apoptosis on colorectal cancer, B-cell lymphoma and other related tumors both in vitro and in vivo by disrupting the binding of RelB to target DNA. RS47 can be used for the research of tumors and infectious diseases.
    RS47
  • HY-N4149
    Quercetagetin
    		Inhibitor 99.94%
    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.
    Quercetagetin
  • HY-18095
    CX-6258
    		Inhibitor 98.06%
    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.
    CX-6258
  • HY-12830
    M-110
    		Inhibitor 99.05%
    M-110 is a highly selective, ATP-competitive inhibitor of PIM kinases with a preference for PIM-3 (IC50=47 nM). M-110 inhibits PIM-1 and PIM-2 with similar IC50s of 2.5 μM. M-110 inhibits the proliferation of prostate cancer cell lines with IC50s of 0.6 to 0.9 μM.
    M-110
  • HY-19322B
    PIM-447 dihydrochloride
    		Inhibitor 99.82%
    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.
    PIM-447 dihydrochloride
  • HY-18086
    TCS PIM-1 1
    		Inhibitor 98.40%
    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-16976
    GDC-0339
    		Inhibitor 99.87%
    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.
    GDC-0339
  • 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.
    CK2/ERK8-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
Pim Isoform Comparison

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