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HDAC inhibition

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-104008
    ACY-957
    1 Publications Verification

    		 HDAC Others
    ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9 .
    ACY-957
  • HY-12164
    Mocetinostat
    10+ Cited Publications

    MGCD0103

    		 HDAC Autophagy Apoptosis Cancer
    Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.
    Mocetinostat
  • HY-119017
    SB-429201

    		HDAC Cancer
    SB-429201 is a potent and selective HDAC1 (IC50~1.5 μM). SB-429201 displays at least a 20-fold preference for HDAC1 inhibition over HDAC3 and HDAC8 .
    SB-429201
  • HY-132998
    HDAC6 degrader-1

    		PROTACs Others
    HDAC6 degrader-1 is a PROTAC that comprises a selective HDAC6 inhibitor Nexturastat A (Nex A) as the HDAC6 binder, a linker and a ligand for recruiting E3 ligase. HDAC6 degrader-1 induces significant degradation of HDAC6, exhibits excellent selectivity against other HDACs, and demonstrates efficient inhibition of cell proliferation .
    HDAC6 degrader-1
  • HY-149819
    CDK/HDAC-IN-3

    		HDAC CDK Cancer
    CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
    CDK/HDAC-IN-3
  • HY-12954
    PTACH

    NCH-51

    		 HDAC HIV Infection Cancer
    PTACH (NCH-51) is a potent HDAC inhibitor with IC50s of 48 nM, 32 nM, and 41 nM for HDAC1, HDAC4, and HDAC6, respectively. PTACH exerts potent growth inhibition against various cancer cells (EC50s of 1.1-9.1 μM) .
    PTACH
  • HY-13909
    RGFP966
    Maximum Cited Publications
    38 Publications Verification

    		 HDAC Cancer
    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
    RGFP966
  • HY-149859
    HDAC-IN-58

    		HDAC Neurological Disease
    HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC50 value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions .
    HDAC-IN-58
  • HY-157889
    ZINC000028464438

    		HDAC Cancer
    ZINC000028464438 is a selective HDAC11 inhibitor with an IC50 of 3.5 µM. ZINC000028464438 shows almost no inhibition for other HDAC subtypes .
    ZINC000028464438
  • HY-169400
    HDACs/EZH2-IN-1

    		HDAC Histone Methyltransferase Apoptosis Cancer
    HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC50: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis .
    HDACs/EZH2-IN-1
  • HY-100585
    Splitomicin

    Splitomycin

    		 HDAC Cancer
    Splitomicin (Splitomycin) is a selective Sir2p inhibitor. Splitomicin inhibits NAD +-dependent HDAC activity of Sir2 protein. Splitomicin induces dose-dependent inhibition of HDAC in the yeast extract with an IC50 of 60 μM .
    Splitomicin
  • HY-121315
    BRD4097

    		HDAC Metabolic Disease
    BRD4097 is an inhibitor of histone deacetylase (HDAC). BRD4097 acts by inhibiting the activity of HDACs, especially HDAC 1,2 and 3, through metal chelation and spatial rejection mechanisms, and this inhibition may help regulate gene expression and alter chromatin structure, thereby affecting a variety of biological processes. BRD4097 is used to study the role of HDAC in cholesterol metabolism and NPC1 diseases .
    BRD4097
  • HY-152225
    MC2625

    		HDAC Apoptosis Cancer
    MC2625 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2625 show selective HDAC3 and HDAC6 inhibition with IC50s of 80 nM and 11 nM. MC2625 increases acetyl-H3 and acetyl-tubulin levels and inhibits cancer stem cells (CSCs) growth by apoptosis induction .
    MC2625
  • HY-162910
    HDAC-IN-79

    		Xanthine Oxidase HDAC Autophagy Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    HDAC-IN-79 (compound 4) is an orally active dual xanthine oxidase-HDAC inhibitor (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM;), with significant in vivo anti-hyperuricemia and anti-tumor activities. HDAC-IN-79 is the most potent cell growth inhibitor (IC50=0.706 μM) of leukemia HL60 cells, induces apoptosis and autophagy, and can regulate the expression levels of signature biomarkers associated with intracellular HDAC inhibition .
    HDAC-IN-79
  • HY-N0071
    Crotonoside

    Isoguanosine

    		 FLT3 HDAC Cancer
    Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the research of AML .
    Crotonoside
  • HY-138831
    AES-350

    		HDAC Apoptosis Cancer
    AES-350 is a potent and orally active HDAC6 inhibitor with an IC50 and a Ki of 0.0244 μM and 0.035 μM, respectively. AES-350 is also against HDAC3, HDAC8 in an enzymatic activity assay with IC50 values of 0.187 μM and 0.245 μM, respectively. AES-350 triggers apoptosis in AML cells through HDAC inhibition and can be used for acute myeloid leukemia (AML) research .
    AES-350
  • HY-153358
    TNG260

    		HDAC Cancer
    TNG260 is a CoREST-selective deacetylase (CoreDAC) inhibitor. TNG260 inhibits HDAC1 with 10-fold selectivity over HDAC3. TNG260 leads to HDAC1 inhibition, reverses anti-PD1 resistance driven by loss of STK11. TNG260 decreases intratumoral infiltration of neutrophils. TNG260 exhibits immune-mediated cell killing .
    TNG260
  • HY-161984
    HDAC-IN-76

    		HDAC Infection Others
    HDAC-IN-76 (compound 6i) is a histone deacetylase (HDAC) inhibitor. HDAC-IN-76 IC50 values of 30 nM and 98 nM for Pf3D7 (chloroquine (HY-17589A) drug-susceptible strain) and PfDd2 (chloroquine (HY-17589A) drug-resistant strain), has a highly potent antimalarial activity against asexual blood-stage Plasmodium, respectively, and exhibits selective inhibition against parasites, with IC50 values of 7 nM and 9 nM for human HDAC1 and HDAC6, respectively, while inhibiting PfHDAC1 .
    HDAC-IN-76
  • HY-150503
    KH-259

    		HDAC Neurological Disease
    KH-259 (compound 1) is a potent, selective and CNS-penetrant HDAC6 inhibitor, with an IC50 of 0.26 μM. KH-259 has antidepressant effects in mice through the inhibition of HDAC6 in the brain. KH-259 can be used for neurodegenerative diseases research .
    KH-259
  • HY-155329
    GK718

    		HDAC Inflammation/Immunology
    GK718 is a HDAC1/3 inhibitor (IC50: 259 and 139 nM respectively). GK718 increased acetylated histone H3 level in cells. GK718 inhibits Bleomycin (HY-108345) induced pulmonary fibrosis in mice .
    GK718
  • HY-13265
    AR-42
    2 Publications Verification

    HDAC-42; OSU-HDAC42

    		 HDAC Autophagy Apoptosis Cancer
    AR-42 (HDAC-42; OSU-HDAC42) is a potent, orally bioavailable pan-HDAC inhibitor (IC50=16 nM). AR-42 induces growth inhibition, cell-cycle arrest, apoptosis, and activation of caspases-3/7. AR-42 promotes hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. AR-42 shows cytotoxicity against various human cancer cell lines .
    AR-42
  • HY-159966
    Top/HDAC-IN-3

    		Topoisomerase HDAC Reactive Oxygen Species Apoptosis Cancer
    Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562) .
    Top/HDAC-IN-3
  • HY-153358A
    (S)-TNG260

    		HDAC Cancer
    (S)-TNG260 is an isomer of TNG260 (HY-153358). TNG260 is a CoREST selective deacetylase (CoreDAC) inhibitor. TNG260 inhibits HDAC1 with 10-fold selectivity over HDAC3. TNG260 causes HDAC1 inhibition and reverses anti-PD1 resistance driven by STK11 deletion. TNG260 reduces intratumoral infiltration of neutrophils. TNG260 exhibits immune-mediated cell killing.
    (S)-TNG260
  • HY-144315
    CYD19

    Snail/HDAC-IN-1

    		 HDAC Cancer
    CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. CYD19 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
    CYD19
  • HY-145406
    IHCH-3064

    		Adenosine Receptor HDAC Inflammation/Immunology Cancer
    IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
    IHCH-3064
  • HY-128436
    KT-531

    		HDAC Cancer
    KT-531 is a potent and selective inhibitor of HDAC6 with an IC50 of 8.5 nM. KT-531 exhibits strong inhibition against SUP-T11 cells with an IC50 of 0.42 μM. KT-531 can be used in study hematological cancers .
    KT-531
  • HY-147730
    HDAC6-IN-8

    		HDAC Cancer
    A variety of compounds were designed and synthesized by modifying cap groups. The enzyme inhibition test showed that compound 12C had broad-spectrum enzyme inhibitory activity, and compounds 9m and 9q were more inclined to inhibit HDAC6, showing a certain selective inhibitory activity among the representative subtypes.
    HDAC6-IN-8
  • HY-118783
    2-Hexyl-4-pentynoic acid

    (±)-2-Hexyl-4-pentynoic acid

    		 HDAC HSP Neurological Disease
    2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), valproic acid (VPA) derivative, exhibits potential roles of HDAC inhibition (IC50=13 μM) and HSP70 induction. Potent neuroprotective effects. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons . 2-Hexyl-4-pentynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    2-Hexyl-4-pentynoic acid

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