Pim

Pim kinase inhibitors act on Pim-1, Pim-2 and Pim-3, constitutively active kinases of cell survival. The name derives from proviral integration sites for Moloney murine leukemia virus, first mapped in 1984 in mouse T cell lymphomas. Pim kinases lack a regulatory domain, so their activity depends mainly on expression downstream of cytokine receptor signaling. Janus kinase (JAK) and signal transducer and activator of transcription (STAT) proteins induce their transcription. The kinases phosphorylate substrates that control apoptosis, protein translation and cell cycle progression, and they cooperate with Myc in tumorigenesis. AZD1208 and CX-6258 inhibit all three isoforms, while SGI-1776 was developed as a Pim-1 inhibitor.

Items 1-25 of 62

  • AZD1208
    Cat. No.
    A13203

    AZD1208

    AZD1208 is orally available, small molecule inhibitor of PIM kinases with potential antineoplastic activity.

    2 mg
    $25.00
    5 mg
    $40.00
    All 9 sizes
  • LGB-321 HCl
    Cat. No.
    A14420

    LGB-321 HCl

    Synonyms: LGB-321

    LGB-321 HCl is a potent and selective ATP-competitive small molecule inhibitor of PIM kinases (Pan-PIM kinase inhibitor).

    Out of stock

    All 3 sizes
  • SGI-1776 (free base)
    Cat. No.
    A10838

    SGI-1776 (free base)

    Synonyms: SGI1776

    SGI-1776 free base is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM in a cell-free assay, 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin. Phase 1.

    2 mg
    $40.00
    5 mg
    $80.00
    All 7 sizes
  • (Z)-SMI-4a
    Cat. No.
    A11945

    (Z)-SMI-4a

    Synonyms: SMI4a

    SIM-4a is a Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK. Mostly potent to Pim-2, does not significantly inhibit any other serine/threonine- or tyrosine-kinases.

    5 mg
    $40.00
    10 mg
    $60.00
    All 6 sizes
  • Pim1/AAK1-IN-1
    Cat. No.
    A11476

    Pim1/AAK1-IN-1

    Synonyms: LKB1/AAK1 dual inhibitor

    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.

    1 mg
    $75.00
    2 mg
    $115.00
    All 8 sizes
  • TCS PIM-1 4a
    Cat. No.
    A11967

    TCS PIM-1 4a (SMI-4a)

    Synonyms: SMI-4a

    TCS PIM-1 4a is a selective and ATP-competitive Pim kinase inhibitor (IC50 values = 24 and 100 nM for Pim-1 and Pim-2, respectively).

    5 mg
    $40.00
    10 mg
    $60.00
    All 7 sizes
  • CX-6258
    Cat. No.
    A12896

    CX-6258

    CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

    1 mg
    $25.00
    5 mg
    $65.00
    All 8 sizes
  • Hispidulin
    Cat. No.
    A13945

    Hispidulin

    Synonyms: Dinatin

    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.

    1 mg
    $25.00
    5 mg
    $55.00
    All 7 sizes
  • CX-6258 HCl
    Cat. No.
    A14275

    CX-6258 HCl

    Synonyms: CX6258

    CX-6258 HCl is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3.

    1 mg
    $30.00
    5 mg
    $75.00
    All 8 sizes
  • CX-6258 hydrochloride hydrate
    Cat. No.
    A15055

    CX-6258 hydrochloride hydrate

    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.

    2 mg
    $75.00
    5 mg
    $85.00
    All 6 sizes
  • TCS PIM-1 1
    Cat. No.
    A15369

    TCS PIM-1 1

    Synonyms: SC 204330

    TCS PIM-1 1 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).

    1 mg
    $25.00
    5 mg
    $50.00
    All 8 sizes
  • PIM447
    Cat. No.
    A16807

    PIM447 (LGH447)

    Synonyms: LGH-447; LGH447 free base

    PIM447 is a novel pan-PIM kinase inhibitor with Ki values of 6 pM, 18 pM, 9 pM for PIM1, PIM2, PIM3 respectively. It also inhibits GSK3β, PKN1, and PKCτ, but at a significantly lower potency with IC50 between 1 and 5 μM (>105-fold differential relative to the Ki on PIMs).

    1 mg
    $110.00
    2 mg
    $155.00
    All 7 sizes
  • AZD1208 HCl
    Cat. No.
    A16927

    AZD1208 HCl

    Synonyms: AZD 1208

    AZD1208 hydrochloride is a novel, orally bioavailable, highly selective PIM kinases inhibitor.

    5 mg
    $45.00
    10 mg
    $65.00
    All 5 sizes
  • SMI-16a
    Cat. No.
    A17157

    SMI-16a

    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.

    1 mg
    $25.00
    2 mg
    $35.00
    All 8 sizes
  • GNE-955
    Cat. No.
    A19243

    GNE-955

    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.

    1 mg
    $315.00
    5 mg
    $955.00
    All 6 sizes
  • PIM1-IN-1
    Cat. No.
    A19392

    PIM1-IN-1

    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.

    1 mg
    $315.00
    5 mg
    $390.00
    All 6 sizes
  • TP-3654
    Cat. No.
    A20584

    TP-3654

    TP-3654 is a second-generation Pim kinase inhibitor with Ki values of 5 and 42 nM for Pim-1 and Pim-3, respectively.

    5 mg
    $45.00
    10 mg
    $70.00
    All 6 sizes
  • GDC-0339
    Cat. No.
    A20920

    GDC-0339

    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.

    2 mg
    $275.00
    5 mg
    $445.00
    All 6 sizes
  • INCB053914 phosphate
    Cat. No.
    A21444

    INCB053914 phosphate

    Synonyms: INCB 053914

    INCB053914 phosphate is an inhibitor of Pim extracted from patent WO 2017044730 A1, compound 1; has an IC50 of less than 35 nM.

    1 mg
    $80.00
    5 mg
    $220.00
    All 6 sizes
  • SEL24-B489
    Cat. No.
    A22203

    SEL24-B489

    Synonyms: MEN1703; SEL24

    SEL24-B489 is a potent, type I, orally active dual inhibitor of PIM kinases and FLT3-ITD. It exhibits high affinity for PIM family members, with Kd values of 2 nM for PIM1, 2 nM for PIM2, and 3 nM for PIM3, making it a promising candidate for targeted cancer therapy.

    1 mg
    $165.00
    5 mg
    $425.00
    All 6 sizes
  • JP-11646
    Cat. No.
    A25140

    JP-11646

    JP-11646 is a potent pan-PIM inhibitor specifically targeting PIM2 with an IC50 of 0.5 nM. This reversible, ATP non-competitive inhibitor significantly reduces the mRNA levels of PIM1, PIM2, and PIM3. JP-11646 has demonstrated efficacy in inhibiting cell viability in small cell lung cancer (SCLC) and large cell neuroendocrine carcinomas of the lung (LCNEC), leading to apoptosis or necroptosis through decreased p-4EBP-1 and altered caspase activity. This reagent is valuable for research applications in SCLC, LCNEC, acute myeloid leukemia (AML), multiple myeloma (MM), and triple-negative breast cancer (TNBC).

    1 mg
    $250.00
    5 mg
    $630.00
    All 6 sizes
  • Pim-1 kinase inhibitor 10
    Cat. No.
    A25155

    Pim-1 kinase inhibitor 10

    Pim-1 kinase inhibitor 10 is a selective inhibitor of PIM-1 and PIM-2 kinases, functioning through both competitive and non-competitive mechanisms. This compound effectively induces apoptosis in cancer cells, demonstrating significant anticancer activity. Additionally, Pim-1 kinase inhibitor 10 activates caspase 3 and 7, further contributing to its potential as a therapeutic agent in cancer research.

    Out of stock

    All 3 sizes
  • IBL-302
    Cat. No.
    A25844

    IBL-302

    Synonyms: AMU302

    IBL-302 is an orally available dual inhibitor targeting PIM and the PI3K/AKT/mTOR pathways. It exhibits significant antitumor activity against breast cancer and neuroblastoma, showing in vivo efficacy in nude mouse xenograft models by overcoming trastuzumab resistance. Additionally, IBL-302 enhances the cytotoxic effects of commonly used chemotherapeutic agents, including cisplatin, doxorubicin, and etoposide, making it a valuable compound for cancer research applications.

    1 mg
    $310.00
    5 mg
    $805.00
    All 4 sizes
  • CRT0066101
    Cat. No.
    A30245

    CRT0066101

    CRT0066101 is a potent and orally active inhibitor of Protein Kinase D (PKD) with IC50 values of 1 nM, 2.5 nM, and 2 nM for PKD1, PKD2, and PKD3, respectively. Additionally, it serves as an effective PIM2 inhibitor with an IC50 of approximately 135.7 nM. This compound exhibits notable anti-inflammatory activity demonstrated in LPS-induced lung injury models in mice, as well as anticancer effects, making it a valuable tool for research in cancer and inflammation-related studies.

    5 mg
    $130.00
    10 mg
    $215.00
    All 2 sizes

Items 1-25 of 62

Added to your cart

View Cart Checkout

    Loading...