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HDAC-IN-2

" in MedChemExpress (MCE) Product Catalog:

63

Inhibitors & Agonists

1

Biochemical Assay Reagents

2

Natural
Products

1

Isotope-Labeled Compounds

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-109015
    Tucidinostat
    Maximum Cited Publications
    34 Publications Verification

    Chidamide; HBI-8000; CS 055

    		 HDAC Cancer
    Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9 .
    Tucidinostat
  • HY-50934
    Tacedinaline
    5+ Cited Publications

    N-acetyldINalINe; CI-994; Goe-5549

    		 HDAC Apoptosis Cancer
    Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.
    Tacedinaline
  • HY-104008
    ACY-957
    2 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-111818
    TH34
    1 Publications Verification

    		 HDAC Cancer
    TH34, an HDAC6/8/10 inhibitor with IC50s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3 .
    TH34
  • HY-19348
    Pimelic Diphenylamide 106
    5 Publications Verification

    RGFA-8; TC-H 106; Histone Deacetylase INhibitor VII

    		 HDAC Monoamine Transporter Neurological Disease Cancer
    Pimelic Diphenylamide 106 (TC-H 106) is a slow, tight binding class I HDAC inhibitor (inhibits HDAC1, 2, and 3 with IC50 values of 150 nM, 760 nM, and 370 nM, respectively), with no activity against class II HDACs. Pimelic Diphenylamide 106 modulates dopamine concentration and protects dopamine cells by inducing VMAT2 expression. Pimelic Diphenylamide 106 can be used in the study of neuropsychiatric diseases such as attention deficit hyperactivity disorder (ADHD) [2] .
    Pimelic Diphenylamide 106
  • HY-119939
    CHDI-390576
    1 Publications Verification

    CHDI00390576

    		 HDAC Cancer
    CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
    CHDI-390576
  • HY-W010516
    2-Methylvaleric acid

    2-Methylpentanoic acid

    		 Endogenous Metabolite Metabolic Disease
    2-Methylvaleric acid is a branched short-chain fatty acid (SCFA) produced by the metabolism of branched-chain amino acids by gut microbes. 2-Methylvaleric acid can be used as a potential biomarker for metabolic diseases such as type 2 diabetes, and its content is significantly reduced in the feces of diabetic mice. 2-Methylvaleric acid may regulate host energy metabolism and inflammatory response through G protein-coupled receptors (GPCRs) or histone deacetylase (HDAC) inhibition. 2-Methylvaleric acid can be used to study gut microbe-host interactions and metabolic diseases as a fecal biomarker[1][2].
    2-Methylvaleric acid
  • HY-110264
    MI-192

    		HDAC Apoptosis Neurological Disease Cancer
    MI-192 is a selective HDAC2 and HDAC3 inhibitor with IC50s of 30 nM and 16 nM, respectively. MI-192 is more selective for HDAC2/3 than other HDAC isomers.MI-192 induces myeloid leukaemic cells apoptosis. Anticaner and neuroprotective activities [2].
    MI-192
  • HY-174444A
    PROTAC HDAC degrader-2 TFA

    		PROTACs HDAC Cancer
    PROTAC HDAC degrader-2 TFA is the trifluoroacetate salt of PROTAC HDAC degrader-2. PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs .
    PROTAC HDAC degrader-2 TFA
  • HY-13592
    HDAC-IN-7

    Chidamide impurity

    		 HDAC Cancer
    HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
    HDAC-IN-7
  • HY-145819
    JPS036

    		PROTACs HDAC Cancer
    JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS036
  • HY-178161
    HDAC degrader-2

    		HDAC Apoptosis Cancer
    HDAC degrader-2 is a selective HDAC degrader with a DC50 values of 2.55 μM against HDAC1. HDAC degrader-2 effectively induces the degradation of HDAC1 and HDAC2, but has no significant effect on the degradation of HDAC3, 4, 6 and 8. HDAC degrader-2 exerts potent antiproliferative effects against MM.1S and MCF-7 cells. HDAC degrader-2 induces apoptosis in myeloma cells. HDAC degrader-2 can be used for the study of myeloma .
    HDAC degrader-2
  • HY-33287
    2-Bromothiazole-5-carboxylic acid

    		Biochemical Assay Reagents Cancer
    2-Bromothiazole-5-carboxylic acid is a starting compound in the synthesis of active compounds. 2-Bromothiazole-5-carboxylic acid can be used in the synthesis of NAMPT/HDAC inhibitors. 2-Bromothiazole-5-carboxylic acid can be used in the research of colon cancer, lung cancer, and liver cancer .
    2-Bromothiazole-5-carboxylic acid
  • HY-145815A
    JPS014 TFA

    		PROTACs HDAC Apoptosis Cancer
    JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS014 TFA
  • HY-124053
    BRD2492

    		HDAC Cancer
    BRD2492 (compound 6d) is a potent, selective HDAC1 and HDAC2 inhibitor with IC50s of 13.2 nM and 77.2 nM, respecrtively. BRD2492 exhibits >100-fold selectivity for HDAC1/2 over selectivity over HDAC3 and HDAC6. BRD2492 inhibits breast cancer cell lines growth with IC50s of 1.01 μM and 11.13 μM for T-47D and MCF-7 cells, respectively .
    BRD2492
  • HY-145259
    HDAC6-IN-3

    		HDAC Histone Demethylase Cancer
    HDAC6-IN-3 (Compound 14), an antiprostate cancer agent, is a potent, orally active HDAC6 inhibitor with IC50s ranging from 0.02-1.54 μM for HDAC1/2/3/6/8/10. HDAC6-IN-3 is also an effective MAO-A (IC50=0.79 μM) and LSD1 inhibitor . HDAC6-IN-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    HDAC6-IN-3
  • HY-175988
    DNMT/HDAC-IN-2

    		DNA Methyltransferase HDAC Cancer
    DNMT/HDAC-IN-2 (Compound Y7) is a DNMT and HDAC inhibitor with IC50 values for DNMT1, HDAC1, and HDAC6 of 365, 0.2, and 8.91 nM respectively. DNMT/HDAC-IN-2 inhibits the proliferation of breast cancer cells. DNMT/HDAC-IN-2 significantly reduces tumor growth in xenografts and transgenic breast cancer mouse models. DNMT/HDAC-IN-2 can be used for the study of breast cancer .
    DNMT/HDAC-IN-2
  • HY-155328
    GK444

    		HDAC Inflammation/Immunology
    GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC50: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC50 of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice .
    GK444
  • HY-115585
    HDAC-IN-2

    		HDAC Others
    HDAC-IN-2 (Compound 6) is an inhibitor of histone deacetylase 4 (HDAC4). HDAC-IN-2 has affinity for Class IIa enzymes. HDAC-IN-2 is a useful research tool for high-throughput screening and follow-up chemistry .
    HDAC-IN-2
  • HY-174444
    PROTAC HDAC degrader-2

    		PROTACs HDAC Cancer
    PROTAC HDAC degrader-2 is a selective IIb HDACs PROTAC degrader, with DC50s of 13 nM for HDAC6, 29 nM for HDAC10, respectively. PROTAC HDAC degrader-2 exhibits low cytotoxicity against hematological and solid cancer cell lines. PROTAC HDAC degrader-2 can be used for the chemical knockdown of class IIb HDACs .
    PROTAC HDAC degrader-2
  • HY-139650
    HDAC1/2-IN-3

    		HDAC Cancer
    HDAC1/2-IN-3 is a HDAC1 and HDAC2 inhibitor with IC50 values 0-5 and 5-10 nM, respectively.
    HDAC1/2-IN-3
  • HY-109015S
    Tucidinostat-d4

    Chidamide-d4; HBI-8000-d4; CS 055-d4

    		 Isotope-Labeled Compounds HDAC Cancer
    Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively .
    Tucidinostat-d4
  • HY-145815
    JPS014

    		PROTACs HDAC Apoptosis Cancer
    JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS014
  • HY-145818
    JPS035

    		PROTACs HDAC Cancer
    JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .
    JPS035
  • HY-175513
    ZWZH-21

    		HDAC Apoptosis Cancer
    ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC50 values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC50 values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer .
    ZWZH-21
  • HY-176561
    IOR-160

    		Casein Kinase HDAC Cancer
    IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research .
    IOR-160
  • HY-146276
    CDK/HDAC-IN-2

    		HDAC CDK Apoptosis Cancer
    CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC50 of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy .
    CDK/HDAC-IN-2
  • HY-174302
    PIM-1/HDAC-IN-2

    		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-145852
    Top/HDAC-IN-2

    		HDAC Topoisomerase Apoptosis Cancer
    Top/HDAC-IN-2 (45b), a Top and HDAC dual inhibitor, exhibits potent antitumor activities and induces apoptosis .
    Top/HDAC-IN-2
  • HY-174398
    GSK-3β/HDAC-IN-2

    		GSK-3 HDAC Tau Protein Neurological Disease
    GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease.
    GSK-3β/HDAC-IN-2
  • HY-143325
    A2AAR/HDAC-IN-2

    		HDAC Adenosine Receptor Cancer
    A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor .
    A2AAR/HDAC-IN-2
  • HY-174471
    HDAC-IN-90

    		HDAC Ligands for Target Protein for PROTAC Cancer
    HDAC-IN-90 is the ligand for HDAC6/10 that can be used for synthesis of PROTAC HDAC degrader-2 (HY-174444) .
    HDAC-IN-90
  • HY-118421
    Nullscript

    		Parasite HDAC Infection
    Nullscript is a negative control for Scriptaid. Nullscript is a known inactive analog of Scriptaid . Scriptaid is a representative HDAC inhibitor . Nullscript inhibits Cryptosporidium (C. parvum) growth with the IC50 value of 2.1 μM .
    Nullscript
  • HY-151569
    SAHA-OH

    		HDAC Apoptosis Inflammation/Immunology
    SAHA-OH is a selective HDAC6 inhibitor (IC50=23 nM), shows a 10- to 47-fold selectivity for HDAC6 compared to HDAC 1, 2, 3, and 8. SAHA-OH shows anti-inflammatory activity, and attenuates macrophage apoptosis .
    SAHA-OH
  • HY-163282
    NB512

    		HDAC Epigenetic Reader Domain Cancer
    NB512 (compound 39a) is a dual inhibitor for BET and HDAC, which exhibits a efficient binding affinity with BRD4 bromodomains and HDAC1/2, with EC50s of 100-400 nM. NB512 exhibits an anti-proliferative activity towards cancer cells PaTu8988T and NMC .
    NB512
  • HY-150577
    HDAC-IN-45

    		HDAC Cancer
    HDAC-IN-45 (Compound 14) is a small molecule HDAC inhibitor and has anticancer activity, also can forms a hydrogen bond with residue Y303. HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively .
    HDAC-IN-45
  • HY-146351
    HDAC-IN-38

    		HDAC Neurological Disease
    HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5) .
    HDAC-IN-38
  • HY-177768
    HDAC-IN-96

    		HDAC Apoptosis Cancer
    HDAC-IN-96 (Compound 3f) is a selective HDAC1/2 inhibitor with IC50 values of 457.1 and 433.7 nM. HDAC-IN-96 has strong inhibitory activity against multiple hematological tumor cells (RS4;11, K562, RPMI-8226, U266), with IC50 values ranging from 2.11 to 5.35 μM. HDAC-IN-96 can induce cancer cells apoptosis and S phase arrest. HDAC-IN-96 can be used for the research of cancer, such as acute lymphoblastic leukemia .
    HDAC-IN-96
  • HY-149283
    JAK/HDAC-IN-2

    		JAK HDAC Apoptosis Cancer
    JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers .
    JAK/HDAC-IN-2
  • HY-175805
    EGFR/HDAC-IN-2

    		EGFR HDAC Apoptosis Cancer
    EGFR/HDAC-IN-2 (Compound 38) is dual-functional inhibitor of EGFR and HDAC3 with IC50s of 20.34 and 1.09 nM for CDK9 and HDAC3, respectively. EGFR/HDAC-IN-2 has superior anti-proliferative activity against cancer cells, inhibits cell migration and induces late-stage cell apoptosis. EGFR/HDAC-IN-2 significantly inhibits triple-negative breast cancer (TNBC) tumor growth in xenograft mouse models. EGFR/HDAC-IN-2 can be used for cancers like TNBC research .
    EGFR/HDAC-IN-2
  • HY-155523
    Tubulin/HDAC-IN-2

    		Microtubule/Tubulin HDAC Apoptosis Cancer
    Tubulin/HDAC-IN-2 (Compound II-19k) is a dual inhibitor of Tubulin and HDAC, with an IC50 of 0.403 μM, 0.591μM, 3.552μM, 0.459μM for HDAC1/2/3/6. Tubulin/HDAC-IN-2 blocks cell cycle arrest at G2 phase, induces cell apoptosis. Tubulin/HDAC-IN-2 inhibits the growth of hematoma and solid tumor cells, reduces tumor metastasis, and also inhibits tumor growth in a liver tumor allograft mouse model .
    Tubulin/HDAC-IN-2
  • HY-162906
    FLT3/HDAC-IN-2

    		HDAC FLT3 Cancer
    FLT3/HDAC-IN-2 is (compound 25h) a FLT3/HDAC dual inhibitor. FLT3/HDAC-IN-2 has antiproliferative activity against MOLM-13 cells. FLT3/HDAC-IN-2 can be used in acute myeloid leukemia research .
    FLT3/HDAC-IN-2
  • HY-149239
    Topo II/HDAC-IN-2

    		Topoisomerase HDAC Apoptosis Cancer
    Topo II/HDAC-IN-2 (8d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-2 (8d) induces apoptosis .
    Topo II/HDAC-IN-2
  • HY-172177
    ROCK/HDAC-IN-2

    		Apoptosis HDAC ROCK Cancer
    ROCK/HDAC-IN-2 (Compound C-9) is a ROCK/HDAC inhibitor, with IC50 values of 0.185 µM, 0.8 µM, and 0.7 µM for HDAC6, ROCK1, and ROCK2, respectively. ROCK/HDAC-IN-2 can induce apoptosis and changes in mitochondrial membrane potential in cancer cells, demonstrating significant antitumor activity. ROCK/HDAC-IN-2 can be used in the research of pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC) .
    ROCK/HDAC-IN-2
  • HY-143462
    c-Met/HDAC-IN-2

    		HDAC c-Met/HGFR Apoptosis Cancer
    c-Met/HDAC-IN-2 is a highly potent c-Met and HDAC dual inhibitor with IC50s of 18.49 nM and 5.40 nM for HDAC1 and c-Met, respectively. c-Met/HDAC-IN-2 has antiproliferative activities against certain cancer cell lines. c-Met/HDAC-IN-2 can cause G2/M-phase arrest and induce apoptosis in HCT-116. c-Met/HDAC-IN-2 can be used for researching anti-cancer resistance .
    c-Met/HDAC-IN-2
  • HY-162828
    STAT3/HDAC-IN-2

    		STAT HDAC Cancer
    STAT3/HDAC-IN-2 (compound 18) is a dual inhibitor of STAT3 and HDAC, inducing autophagy and apoptosis. STAT3/HDAC-IN-2 is an amphiphilic hydroxamic acid hybrid based on the natural product isopropanol lactone (IAL) and is a nanoscale anticancer agent. STAT3/HDAC-IN-2 can self-assemble in water to form nanoparticles, which have higher tumor tissue accumulation, cellular uptake and anticancer properties compared to the free state .
    STAT3/HDAC-IN-2
  • HY-169938
    LSD1/HDAC-IN-2

    		HDAC Histone Demethylase Apoptosis Cancer
    LSD1/HDAC-IN-2 (Compound 20c) is the inhibitor for LSD and HDAC, that inhibits LSD1, HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with IC50s of 39.0, 1.4, 1.0, 1.3, 2.9 and 16.0 nM, respectively. LSD1/HDAC-IN-2 inhibits the proliferation of cancer cells, especially the colorectal cancer cells. LSD1/HDAC-IN-2 arrests the cell cycle at G2/M phase, inhibits cell migration, and induces apoptosis in HCT-116 and HT-29 cells. LSD1/HDAC-IN-2 exhibits antitumor efficacy in mouse model without significant toxicity .
    LSD1/HDAC-IN-2
  • HY-146159
    PI3K/HDAC-IN-2

    		PI3K HDAC Cancer
    PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC50s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC50s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects .
    PI3K/HDAC-IN-2
  • 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-143497
    HDAC1/2 and CDK2-IN-1

    		HDAC CDK Apoptosis Cancer
    HDAC1/2 and CDK2-IN-1 (compound 14d) is a potent HDAC1, HDAC2 and CDK2 dual inhibitor, with IC50 values of 70.7, 23.1 and 0.80 μM, respectively. HDAC1/2 and CDK2-IN-1 can block the cell cycle and induce apoptosis. HDAC1/2 and CDK2-IN-1 exhibits desirable in vivo antitumor activity .
    HDAC1/2 and CDK2-IN-1

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