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Pathways Recommended: Stem Cell/Wnt Cell Cycle/DNA Damage
Results for "

THP-1 leukemia cells

" in MedChemExpress (MCE) Product Catalog:

36

Inhibitors & Agonists

1

Peptides

2

Natural
Products

1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-174497
    eGFP mRNA

    		mRNA Others
    eGFP mRNA expresses green fluorescent protein derived from the jellyfish Aequorea victoria. eGFP is a commonly used direct-detection reporter gene in mammalian cell culture, which produces bright green fluorescence. This product is synthesized without modified nucleosides, with a Cap1 version cap analog at the 5' end and a 100nt PolyA tail at the 3' end. It can be used as a positive reference for IVT (in vitro transcription) or LNP delivery systems.
    eGFP mRNA
  • HY-155175
    TIM-3-IN-2

    		Tim3 IFNAR Cancer
    TIM-3-IN-2 is a TIM-3 inhibitor. TIM-3-IN-2 blocks the interactions of TIM-3 with PtdSer, CEACAM1 and Gal-9, and inhibits the immunosuppressive function of TIM-3. TIM-3-IN-2 restores IFNγ release from peripheral blood mononuclear cells. TIM-3-IN-2 inhibits the proliferation of acute myeloid leukemia cells. TIM-3-IN-2 can be used for the research of acute myeloid leukemia .
    TIM-3-IN-2
  • HY-12475
    Mutant IDH1-IN-1
    2 Publications Verification

    Agios 135

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Mutant IDH1-IN-1 (Agios 135) is a selective mutant IDH1 inhibitor with activity against both IDH1 R132H and IDH1 R132C. Mutant IDH1-IN-1 reduces the level of 2-hydroxyglutarate (2-HG), stabilizes mutant IDH1 protein, and restores blocked monocyte differentiation. Mutant IDH1-IN-1 can be used in tumor-related research .
    Mutant IDH1-IN-1
  • HY-141539
    SETDB1-TTD-IN-1
    5 Publications Verification

    		 Histone Methyltransferase Akt Cancer
    SETDB1-TTD-IN-1 is a SETDB1 methyltransferase activator and SETDB1-TTD competitive inhibitor (Kd of 88 nM), and selectivity for SETDB1-TTD over other tudor and bromodomain proteins. SETDB1-TTD-IN-1 stimulates methyltransferase activity via increased catalytic activity, promotes Akt1 Lys64 methylation, Akt1 Thr308 phosphorylation and activation. SETDB1-TTD-IN-1 prevents SETDB1-TTD-histone H3 peptide association, induces global gene expression changes, exhibits cellular target engagement, and acts as a tool compound for SETDB1-TTD function exploration. SETDB1-TTD-IN-1 can be used for the research of breast cancer .
    SETDB1-TTD-IN-1
  • HY-158341
    IOX5

    		HIF/HIF Prolyl-Hydroxylase Apoptosis Cancer
    IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC50 of 0.19 μM for PHD2. IOX5 stabilizes HIF-1α in acute myeloid leukemia (AML) cells, inhibits cell proliferation and induces apoptosis. IOX5 has anti-leukemia activity .
    IOX5
  • HY-138617
    AI-10-47
    1 Publications Verification

    		 RUNX Cancer
    AI-10-47 is a small molecule inhibitor of CBFβ-RUNX binding, with an IC50 of 3.2 μM .
    AI-10-47
  • HY-153775
    UC-764864

    		E1/E2/E3 Enzyme Apoptosis Cancer
    UC-764864 is a selective UBE2N inhibitor. UC-764864 covalently binds UBE2N catalytic Cys87, blocks ubiquitin-UBE2N thioester formation and polyubiquitin chain synthesis. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates, and induces cell apoptosis. UC-764864 can be used for the research of acute myeloid leukemia .
    UC-764864
  • HY-133136
    PROTAC BRD4 Degrader-2

    		PROTACs Epigenetic Reader Domain Cancer
    PROTAC BRD4 Degrader-2 is a PROTAC connected by ligands for Cereblon and BRD4 with an IC50 of 14.2 nM against BRD4 BD1 .
    PROTAC BRD4 Degrader-2
  • HY-173422
    MS2133

    		PROTACs Histone Methyltransferase Cancer
    MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC50: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)) .
    MS2133
  • HY-135664
    hDHODH-IN-5

    		Dihydroorotate Dehydrogenase DNA/RNA Synthesis Cancer
    DHODH-IN-7 is a human dihydroorotate dehydrogenase (DHODH) inhibitor, with an IC50 of 0.91 μM. DHODH-IN-7 induces differentiation in acute myeloid leukemia .
    hDHODH-IN-5
  • HY-N8390
    3-Epidehydropachymic acid

    		Others Cancer
    3-Epidehydropachymic acid, a lanostane triterpenoid, shows totoxicity effect against human acute monocytic leukemia cell line THP-1 (IC50=52.51 μM) .
    3-Epidehydropachymic acid
  • HY-162658
    Leuxinostat

    		HDAC Apoptosis Cancer
    Leuxinostat is an inhibitor for HDAC with IC50 of 30 nM for hHDAC6. Leuxinostat inhibits the proliferation of cells THP1, K562, U937 and MEK1, induces apoptosis in leukemia cells NB4 and MOLT-4. Leuxinostat inhibits the expansion of hematopoietic stem cells and exhibits antileukemic activity in zebrafish models .
    Leuxinostat
  • HY-147609
    CSF1R-IN-8

    		c-Fms Cancer
    CSF1R-IN-8 (Compound 22) is a CSF-1R inhibitor with an IC50 of 0.012 μM .
    CSF1R-IN-8
  • HY-147611
    CSF1R-IN-10

    		c-Fms Cancer
    CSF1R-IN-10 (Compound 48) is a CSF-1R inhibitor with an IC50 of 0.005 μM .
    CSF1R-IN-10
  • HY-76293
    I2906
    1 Publications Verification

    		 Bacterial Infection
    I2906 is an orally active isocitrate lyase (ICL) inhibitor with a Mycobacterium tuberculosis IC50 of 134.3 μg/mL. I2906 inhibits the growth of Mycobacterium tuberculosis. I2906 can be used for the research of tuberculosis .
    I2906
  • HY-146283
    LSD1-IN-18

    		Histone Demethylase Cancer
    LSD1-IN-18 (compound 7) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.156 μM and KD of 0.075 μM, respectively. LSD1-IN-18 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.16 and 0.21 μM, respectively .
    LSD1-IN-18
  • HY-146284
    LSD1-IN-19

    		Histone Demethylase Cancer
    LSD1-IN-19 (compound 29) is a potent, non-covalent and selective LSD1 inhibitor, with Ki of 0.108 μM and KD of 0.068 μM, respectively. LSD1-IN-19 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.17 and 0.40 μM, respectively .
    LSD1-IN-19
  • HY-146285
    LSD1-IN-20

    		Histone Demethylase Histone Methyltransferase Cancer
    LSD1-IN-20 (compound 1) is a potent dual non-covalent LSD1/G9a inhibitor, with Ki values of 0.44 and 0.68 μM, respectively. LSD1-IN-20 shows antiproliferative activity in THP-1 leukemia cells and MDA-MB-231 breast cancer cells, with IC50 (72 h) of 0.51 and 1.60 μM, respectively .
    LSD1-IN-20
  • HY-P11019
    IS4

    		CXCR Calcium Channel Cancer
    IS4 is a selective CXCR4 competitive antagonist, with an IC50 of 0.65 nM in THP-1 cells and 38.75 nM in Jurkat cells. IS4 is stable in serum and non-cytotoxic. IS4 competitively binds to CXCR4 with CXCL12, thereby inhibiting CXCL12-induced intracellular Ca 2+ release and cancer cell migration. IS4 can be used in the research on the prevention of metastasis of breast cancer, prostate cancer, leukemia, and other diseases .
    IS4
  • HY-155245
    A09-003

    		CDK Bcl-2 Family Cancer
    A09-003 is a CDK-9 inhibitor (IC50: 16 nM). A09-003 inhibits leukemia cell proliferation (IC50: 1.90, 0.86, 2.49, 1.84, 0.48 μM for BDCM, Molm-14, THP-1, U937, MV4-11 cells). A09-003 induces apoptosis and decreases Mcl-1 expression through Thr163 dephosphorylation .
    A09-003
  • HY-173123
    LSD1-IN-40

    		Histone Demethylase Apoptosis Cancer
    LSD1-IN-40 (Compound 9e) is a potent LSD1 inhibitor, with an IC50 of 9.85 nM. LSD1-IN-40 exhibits exceptional selectivity for LSD1 over both MAOs and hERG. LSD1-IN-40 exhibits significant inhibitory activity against leukemia cells (MV-4-11, HL-60, and THP-1 cells). LSD1-IN-40 can induce apoptosis in MV-4-11 cells. LSD1-IN-40 has the potential for the research of acute myeloid leukemia .
    LSD1-IN-40
  • HY-124693
    DB1055

    		Apoptosis Cancer
    DB1055 is a HOXA9 inhibitor that competes with HOXA9 binding to DNA (blocking its DNA interaction activity). DB1055 induces in vitro cell growth reduction, cell apoptosis, and differentiation in human acute myeloid leukemia (AML) cells. DB1055 leads to monocyte-to-macrophage differentiation and exhibits antileukemic activities in a human THP-1 AML in vivo model. DB1055 does not impact human CD34+ bone marrow cells. DB1055 can be used for the research of acute myeloid leukemia[1].
    DB1055
  • HY-147610
    CSF1R-IN-9

    		c-Fms Cancer
    CSF1R-IN-9 (Compound 46) is a CSF-1R inhibitor with an IC50 of 0.028 μM .
    CSF1R-IN-9
  • HY-N1117
    Tristin

    		Phosphatase NO Synthase Infection Metabolic Disease Cancer
    Tristin is a PTP1B inhibitor (IC50=21.2 μM) with antioxidant and antifungal activities. Tristin inhibits lipid peroxidation and NO production in LPS-stimulated macrophages, and also exhibits activity against a variety of phytopathogenic fungi. Tristin is also able to inhibit cancer cell proliferation. Tristin can be used in the research of diseases associated with phytopathogenic fungal infection, leukemia, type 2 diabetes and inflammatory responses .
    Tristin
  • HY-181587
    PDGFRA/CAIX/XII-IN-1

    		PDGFR Carbonic Anhydrase STAT Akt ERK Apoptosis Caspase Cancer
    PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia .
    PDGFRA/CAIX/XII-IN-1
  • HY-182957
    MNK/PIM-IN-2

    		MNK Pim Apoptosis Caspase Eukaryotic Initiation Factor (eIF) PARP c-Myc Cancer
    MNK/PIM-IN-2 is a Mnk/Pim kinase inhibitor with an IC50 of 32 nM for Mnk1, 3 nM for Mnk2, and 37 nM for Pim1. MNK/PIM-IN-2 reduces the levels of p-eIF4E and p-4EBP1. MNK/PIM-IN-2 induces cell cycle arrest, apoptosis (apoptosis) and exerts antiproliferative effects in leukemia cells. MNK/PIM-IN-2 can be used in studies related to leukemia .
    MNK/PIM-IN-2
  • HY-183739
    CQ31

    		Pyroptosis Caspase Cancer
    CQ31 is a PEPD and XPNPEP1 inhibitor, with an IC50 of 0.67 μM against PEPD and an IC50 of 122 μM against XPNPEP1. CQ31 inhibits the M24B aminopeptidase activity of PEPD and XPNPEP1. CQ31 induces the accumulation of Xaa-Pro-containing peptides, mildly inhibits DPP8/9, and triggers CASP1-dependent pyroptosis via activation of the CARD8 inflammasome and caspase-1. CQ31 can be used in research related to cancers such as acute myeloid leukemia .
    CQ31
  • HY-182355
    MTHFD2-IN-7

    		Methylenetetrahydrofolate Dehydrogenase (MTHFD) Cancer
    MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .
    MTHFD2-IN-7
  • HY-181685
    LAGi-DEL

    		LAG-3 TNF Receptor Cancer
    LAGi-DEL is a LAG-3 inhibitor, with Kd values of 97.33 nM and 271 nM in surface plasmon resonance (SPR) assay and microscale thermophoresis (MST) assay, respectively. LAGi-DEL blocks the LAG-3/MHC-II interaction, with an EC50 of 138 nM. LAGi-DEL restores T cell activation, enhances IFN-γ secretion and promotes immune-mediated cytotoxicity. LAGi-DEL can be used in the research of acute myeloid leukemia, lung cancer and melanoma .
    LAGi-DEL
  • HY-148014
    TH7299

    		Methylenetetrahydrofolate Dehydrogenase (MTHFD) Parasite Apoptosis DNA/RNA Synthesis Infection Cancer
    TH7299 is a TbFolD inhibitor with antiparasitic activity. TH7299 binds the tetrahydrofolate-binding pocket of MTHFD2, and inhibits MTHFD2L and the dehydrogenase/cyclohydrolase domain of MTHFD1. TH7299 reduces cancer cells viability, induces apoptosis, DNA damage. TH7299 can be used for the researches of african trypanosomiasis and acute myeloid leukemia.
    TH7299
  • HY-181767
    PROTAC HDAC3 degrader-1

    		PROTACs HDAC Bcl-2 Family Apoptosis Cancer
    PROTAC HDAC3 degrader-1 is a selective PROTAC degrader targeting HDAC3 with a DC50 of 30.73 nM. PROTAC HDAC3 degrader-1 induces degradation of HDAC3 via the ubiquitin-proteasome system. PROTAC HDAC3 degrader-1 promotes apoptosis, induces DNA damage, and downregulates anti-apoptotic proteins Mcl-1 and Bcl-xL. PROTAC HDAC3 degrader-1 can be used for the research of acute myeloid leukemia .
    PROTAC HDAC3 degrader-1
  • HY-119159
    AS1604498

    		NAMPT Caspase Apoptosis Cancer
    AS1604498 is a highly specific competitive inhibitor of human NAMPT, with an IC50 of 44.4 nM. AS1604498 functionally inhibits NAMPT enzymatic activity, reduces nicotinamide mononucleotide production, decreases intracellular NAD levels, activates caspase 3/7 and induces cancer cell apoptosis. AS1604498 is applicable to research related to chronic myeloid leukemia .
    AS1604498
  • HY-183265
    GO847

    		Creatine Kinase ATP Synthase Mitochondrial Metabolism Reactive Oxygen Species (ROS) Cancer
    GO847 is an orally active casein kinase 2 (CK2) inhibitor with an IC50 of 40.2 nM. GO847 increases intracellular ATP levels, impairs Mitochondrial metabolic flexibility, and promotes excessive mitochondrial ROS production. GO847 alters the period length of cellular circadian rhythms. GO847 inhibits the growth of acute myeloid leukemia cells. GO847 can be used for the research of acute myeloid leukemia .
    GO847
  • HY-182349
    Bax activator-2

    		Bcl-2 Family Cancer
    Bax activator-2 (compound 27c) is a pro-apoptotic agent targeting BAX, with an IC50 of 0.30 μmol/L against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, caspase-3/9 cleavage and PARP cleavage, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against various cancer cell lines, shows reduced cytotoxicity in BAX-knockout A549 cells, and has low cytotoxicity against non-cancerous cell lines. Bax activator-2 can be used in studies related to acute myeloid leukemia and solid tumors .
    Bax activator-2
  • HY-111165
    SNX-7081

    		HSP NF-κB ERK JNK PDGFR c-Myc DNA/RNA Synthesis Apoptosis Inflammation/Immunology Cancer
    SNX-7081 is an Hsp90 inhibitor with Ki and IC50 values of 26 nM and 44 nM, respectively. SNX-7081 blocks the nuclear translocation of NF-κB, inhibits the production of pro-inflammatory cytokines, attenuates the ERK/JNK and PDGF signaling pathways, and suppresses LPS (HY-D1056)-induced nitric oxide production. SNX-7081 inhibits DNA repair, induces G2/M cell cycle arrest, and triggers apoptosis via downregulation of MYC/nucleolin and activation of Fas. SNX-7081 can be used in research related to rheumatoid arthritis and cancer .
    SNX-7081
  • HY-185207
    CQ80

    		Pyroptosis Infection Cancer
    CQ80 is a PEPD/XPNPEP1 inhibitor and selective CARD8 inflammasome activator. CQ80 has IC50 values of 0.91 μM for PEPD, 43 μM for XPNPEP1. CQ80 promotes the accumulation of Xaa-Pro peptides by inhibiting PEPD and XPNPEP1, releases the fragment of CARD8 for inflammasome formation, and induces pyroptosis via GSDMD cleavage. CQ80 can be used for research on inflammasome, CARD8-expressing cancer cells, HIV-1-infected cell clearance, acute myeloid leukemia (AML) .
    CQ80

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