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synthesis-and-biological-evaluation-of-pyrazolo-1-5-a-pyrimidine-compounds-as-potent-and-selective-pim-1-inhibitors

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-18095
    CX-6258
    3 Publications Verification

    Pim Cancer
    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-19322B
    PIM-447 dihydrochloride
    5+ Cited Publications

    LGH447 dihydrochloride

    Pim Apoptosis Cancer
    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-16576A
    SMI-4a
    1 Publications Verification

    TCS-pim-1-4a

    Pim Cancer
    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-10371
    Pim1/AAK1-IN-1
    Maximum Cited Publications
    12 Publications Verification

    LKB1/AAK1 dual inhibitor

    Pim Cancer
    Pim1/AAK1-IN-1 is a potent multi-kinase inhibitor with Kd values of 35 nM/53 nM/75 nM/380 nM for Pim1/AAK1/MST2/LKB1 respectively, and also inhibits MPSK1 and TNIK.
    Pim1/AAK1-IN-1
  • HY-78428

    CDK Cancer
    CDK-IN-6, a class of pyrazolo[1,5-a]pyrimidine compound, is a CDK inhibitor with anticancer activities .
    CDK-IN-6
  • HY-18086
    TCS PIM-1 1
    4 Publications Verification

    SC 204330

    Pim Cancer
    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-19322
    PIM447
    5+ Cited Publications

    LGH447

    Pim Apoptosis Cancer
    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-101947
    SMI-16a
    5+ Cited Publications

    pim1/2 Kinase Inhibitor VI

    Pim Cancer
    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.
    SMI-16a
  • HY-W003486

    Phosphodiesterase (PDE) Neurological Disease Cancer
    5,7-Dichloropyrazolo[1,5-a]pyrimidine is a PDE10A inhibitor with a Ki of 24 μM. 5,7-Dichloropyrazolo[1,5-a]pyrimidine serves as a key intermediate in the synthesis of 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives (HIV-1 non-nucleoside reverse transcriptase inhibitors). 5,7-Dichloropyrazolo[1,5-a]pyrimidine can be used for the research of schizophrenia .
    5,7-Dichloropyrazolo[1,5-a]pyrimidine
  • HY-18095A
    CX-6258 hydrochloride hydrate
    3 Publications Verification

    Pim Cancer
    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-40350

    Biochemical Assay Reagents Others
    2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine
  • HY-108605

    Pim Cancer
    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-147785
    Pim-1 kinase inhibitor 2
    1 Publications Verification

    Pim Caspase Bcl-2 Family Apoptosis Cancer
    Pim-1 kinase inhibitor 2 is a PIM-1 kinase inhibitor with a human IC50 of 0.63 μM. Pim-1 kinase inhibitor 2 exhibits high selectivity for cancer cells over normal cells. Pim-1 kinase inhibitor 2 induces apoptosis, increases active caspase-3 levels, upregulates BAX, downregulates Bcl-2, and elevates the Bax/Bcl-2 ratio. Pim-1 kinase inhibitor 2 suppresses cancer cell proliferation and induces cell cycle arrest. Pim-1 kinase inhibitor 2 can be used for the research of prostate carcinoma, hepatocellular carcinoma, and breast adenocarcinoma .
    Pim-1 kinase inhibitor 2
  • HY-Y0519

    Endogenous Metabolite Neurological Disease Cancer
    Pyrimidine is a nitrogen-containing heterocyclic compound and endogenous metabolite. Pyrimidine derivatives can be used in pancreatic cancer, triple-negative breast cancer, colon carcinoma and neuron research .
    Pyrimidine
  • HY-131576A

    dTDP sodium

    Endogenous Metabolite Metabolic Disease
    Thymidine 5′-diphosphate (dTDP) sodium is the key product of pyrimidine synthesis in organisms. Thymidine 5′-diphosphate sodium is produced by thymidylate kinase (TMPK) catalyzed phosphorylation of 5′-thymidine monophosphate (dTMP), which requires ATP and Mg 2+. Thymidine 5′-diphosphate sodium is further catalyzed by TMPK to thymidine 5′-triphosphate (dTTP). TMPK activity can be detected by measuring the level of Thymidine 5′-diphosphate .
    Thymidine 5′-diphosphate sodium
  • HY-W018744

    Biochemical Assay Reagents Others
    2,6-Dichloro pyrimidine -4-amine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    4-Amino-2,6-dichloropyrimidine
  • HY-18095B
    CX-6258 hydrochloride
    3 Publications Verification

    Pim Cancer
    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-111552

    Pim Cancer
    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-W412264

    Pim Cancer
    Pim-1/2 kinase inhibitor 1 is an orally active pim-1/2 kinase inhibitor. Pim-1/2 kinase inhibitor 1 blocks the ability of Pim kinases to phosphorylate peptides, and inhibits the pim protein kinase directed phosphorylation of 4E-BP1 and p27 Kip1. Pim-1/2 kinase inhibitor 1 can be used in study of cancer, especially prostate cancer .
    Pim-1/2 kinase inhibitor 1
  • HY-W017930

    5,7-dichloro-[1,3]thiazolo[5,4-d]pyrimidine

    Drug Intermediate Others
    5,7-Dichlorothiazolo[5,4-d]pyrimidine (5,7-dichloro-[1,3]thiazolo[5,4-d]pyriMidine) is a building block in the chemical synthesis.
    5,7-Dichlorothiazolo[5,4-d]pyrimidine
  • HY-W002404

    Biochemical Assay Reagents Others
    Pyrimidine-4-carboxylic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Pyrimidine-4-carboxylic acid
  • HY-142696A

    CDK Pim Apoptosis Cancer
    CDK6/PIM1-IN-1 (Compound 51) hydrochloride is an orally active and potent dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 hydrochloride inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 hydrochloride significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity .
    CDK6/PIM1-IN-1 hydrochloride
  • HY-123141

    Pim Cancer
    K00135 is a potent and selective inhibitor of PIM kinases. K00135 inhibits survival and clonogenic growth of acute leukemia cells. K00135 inhibits the phosphorylation of PIM downstream targets .
    K00135
  • HY-131576

    dTDP

    Endogenous Metabolite Metabolic Disease
    Thymidine 5′-diphosphate (dTDP) is a key product for pyrimidine synthesis in organisms. Thymidine 5′-diphosphate is generated via the phosphorylation of thymidine 5'-monophosphate (dTMP) catalyzed by thymidylate kinase (TMPK), a process requiring ATP and Mg 2+. Thymidine 5′-diphosphate is further catalyzed by TMPK into thymidine 5'-triphosphate (dTTP). Detection of Thymidine 5′-diphosphate levels enables the assessment of TMPK activity .
    Thymidine 5′-diphosphate
  • HY-150731

    Pim Cancer
    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-142696

    CDK Pim Apoptosis Cancer
    CDK6/PIM1-IN-1 is a potent and balanced dual CDK6/PIM1 inhibitor with IC50 values of 39 and 88 nM, respectively. CDK6/PIM1-IN-1 inhibits CDK4 (IC50=3.6 nM). CDK6/PIM1-IN-1 significantly inhibits acute myeloid leukemia (AML) cell proliferation, arrest cell cycle at the G1 phase, and promote cell apoptosis. CDK6/PIM1-IN-1 exhibits potent anti-AML activity .
    CDK6/PIM1-IN-1
  • HY-162006

    Pim Apoptosis Autophagy Metabolic Disease Inflammation/Immunology Cancer
    Pim-1 kinase inhibitor 8 is a potent PIM-1 inhibitor with an IC50 value of 14.3 nM. Pim-1 kinase inhibitor 8 impedes cell proliferation and migration through PIM-1 inhibition and the induction of both apoptosis and autophagy. Pim-1 kinase inhibitor 8 inhibits solid tumor growth in Solid Ehrlich Carcinoma (SEC)-bearing mice. Pim-1 kinase inhibitor 8 can be used for breast and liver cancer research .
    Pim-1 kinase inhibitor 8
  • HY-69077

    Drug Intermediate Infection
    5-Bromo-1H-pyrazolo[3,4-b]pyridine is a drug intermediate that can be used for the synthesis of sulfonamide derivatives.
    5-Bromo-1H-pyrazolo[3,4-b]pyridine
  • HY-42045

    Drug Derivative Others
    Pyrimidine-5-boronic acid pinacol ester is a derivative of Boronic acid. Boronic acid is an intermediate commonly used in organic synthesis reactions and can be used as a key reagent in the Suzuki-Miyaura reaction. It generates organic free radicals through oxygen-mediated oxidation and exhibits potential mutagenic activity. Boronic acid is mainly used in research in the fields of drug synthesis and catalytic reactions. Pyrimidine-5-boronic acid pinacol ester serves as a building block in DNA-compatible one-pot click chemistry for synthesis of DNA-encoded libraries .
    Pyrimidine-5-boronic acid pinacol ester
  • HY-W017769

    Pyrimidin-4-ylmethanamine

    Drug Intermediate Others
    4-Pyrimidine methanamine (Pyrimidin-4-ylmethanamine) is a synthetic intermediate useful for pharmaceutical synthesis.
    4-Pyrimidine methanamine
  • HY-42697

    Drug Intermediate Others
    (R)-Phenyl (5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)carbamate is a drug intermediate for synthesis of various active compounds.
    (R)-Phenyl (5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)carbamate
  • HY-143898

    Pim Cancer
    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-41832

    Biochemical Assay Reagents Drug Intermediate Cancer
    4,6-Dichloro-2-(methylthio)pyrimidine is an intermediate. 4,6-Dichloro-2-(methylthio)pyrimidine can be used to synthesize Kras modulators. 4,6-Dichloro-2-(methylthio)pyrimidine can be used in cancer research .
    4,6-Dichloro-2-(methylthio)pyrimidine
  • HY-Y0519R

    Reference Standards Endogenous Metabolite Metabolic Disease
    Pyrimidine (Standard) is the analytical standard of Pyrimidine. This product is intended for research and analytical applications. Pyrimidine is a nitrogen-containing heterocyclic compound and endogenous metabolite. Pyrimidine derivatives can be used in pancreatic cancer, triple-negative breast cancer, colon carcinoma and neuron research .
    Pyrimidine (Standard)
  • HY-142656

    Pim Cancer
    PIM-IN-1 is a pan-PIM kinase inhibitor (KG-1, EC50 = 61 nM; pS6, EC50 = 71 nM).
    PIM-IN-1
  • HY-112505

    BCRP Cancer
    Efflux inhibitor-1 (compound 2) is a pyrazolo[1,5-a]pyrimidine efflux inhibitor. Efflux inhibitor-1 selectively targets toward ABCG2/BCRP over ABCB1 with IC50s of 0.45 μM and 2.17 μM, respectively .
    Efflux inhibitor-1
  • HY-78337

    Biochemical Assay Reagents Others
    Methyl pyrimidine-2-carboxylate is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Methyl pyrimidine-2-carboxylate
  • HY-178443

    Pim Apoptosis Cancer
    Pim-1 kinase-IN-15 (Compound 15) is a highly potent and selective Pim-1 kinase inhibitor (IC50=0.212 μM). Pim-1 kinase-IN-15 induces tumor cell apoptosis and suppresses cell migration. Pim-1 kinase-IN-15 is promising for research of oncology, such as breast cancer .
    Pim-1 kinase-IN-15
  • HY-147920

    Pim Cancer
    PIM1-IN-6 (compound 5h) is a potent PIM-1 inhibitor, with an IC50 of 0.60 μM. PIM1-IN-6 shows the high cytotoxicity activity against HCT-116 and MCF-7 cells, with IC50 values of 1.51 and 15.2 μM, respectively .
    PIM1-IN-6
  • HY-78248

    Biochemical Assay Reagents Others
    4-(1H-Pyrazol-4-yl)-7-[[2-(trimethylsilyl)ethoxy]methyl]-7H-pyrrolo[2,3-d]pyrimidine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    4-(1H-Pyrazol-4-yl)-7-[[2-(trimethylsilyl)ethoxy]methyl]-7H-pyrrolo[2,3-d]pyrimidine
  • HY-162059

    Pim Apoptosis Caspase Cancer
    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
  • HY-157404

    Pim Cancer
    Pim-1/2 kinase inhibitor 2 (compound 5b) is a competitive PIM-1 and PIM-2 kinase inhibitor with IC50s of 1.31 μM and 0.67 μM, respectively. Pim-1/2 kinase inhibitor 2 shows in-vitro low cytotoxicity against normal human lung fibroblast Wi-38 cell line and potent in-vitro anticancer activity against myeloid leukaemia (NFS-60), liver (HepG-2), prostate (PC-3), and colon (Caco-2) cancer cell lines .
    Pim-1/2 kinase inhibitor 2
  • HY-174302

    Pim HDAC PARP Apoptosis Cancer
    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-W284026

    Drug Derivative 5-HT Receptor Dopamine Receptor Adrenergic Receptor Neurological Disease
    PIM-35 is a derivative of Indole (HY-W001132). PIM-35 significantly inhibits serotonin (5HT) and dopamine (DA) uptake with a weak inhibitory effect on noradrenaline (NA) uptake.PIM-35 has antidepressant activity and can be used for depression research .
    PIM-35
  • HY-W000643

    Biochemical Assay Reagents Others
    1H-Pyrazolo[3,4-b]pyridine is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    7-Azaindazole
  • HY-W052249

    Biochemical Assay Reagents Others
    1-Methyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
    1-Methyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one
  • HY-52102

    Drug Intermediate Others
    2-(Chloromethyl)pyrimidine hydrochloride is a synthetic intermediate useful for pharmaceutical synthesis.
    2-(Chloromethyl)pyrimidine hydrochloride
  • HY-178133

    Pim Apoptosis Caspase Cancer
    Pim-1 kinase-IN-14 is a PIM-1 kinase inhibitor with an IC50 value of 94 nM. Pim-1 kinase-IN-14 shows broad-spectrum and high-efficiency anticancer activity against multiple human cancer cell lines, including liver cancer (HepG-2), colon cancer (Caco-2), myeloid leukemia (NFS-60), and prostate cancer (PC-3) cells. Pim-1 kinase-IN-14exerts its anticancer effects by inducing apoptosis and activating caspase 3/7. Pim-1 kinase-IN-14 can be used for the study of cancers associated with PIM-1 kinase overexpression .
    Pim-1 kinase-IN-14
  • HY-143295

    Pim Apoptosis Cancer
    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-13287A

    Pim Apoptosis Autophagy Inflammation/Immunology Cancer
    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

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