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HDAC

Items 1-50 of 489

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  1. A12758
    Citarinostat (ACY-241)

    HDAC6 inhibitor

    ACY-241 is a new, selective and orally available inhibitor of HDAC6.
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  2. A11153
    CUDC-907 (Fimepinostat)

    PI3K/HDAC inhibitor

    CUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.
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  3. A10560
    MC1568

    HDAC Inhibitor

    MC1568 is a member of HDAC inhibitors that inhibits the histone deacetylase class II by modifying the genetic expression of various important genes of cell cycle mostly at G1 phase, resulting in the death of breast cancer cells by apoptosis.
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  4. A10611
    MS-275 (Entinostat)

    HDAC inhibitor

    MS-275 (Entinostat) is a potent HDAC inhibitor with IC50 of 0.3 and 8uM for HDAC1 and HDAC3, respectively.
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  5. A11920
    Romidepsin (FK228 ,Depsipeptide)

    HDAC inhibitor

    Romidepsin strongly inhibits HDAC1 and HDAC2 with IC5N/A of 1.6 nM and 3.9 nM, respectively, but is relatively weak in inhibiting HDAC4 and HDAC6 with IC5N/A 25 nM and 79N/A nM, respectively.
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  6. A17323
    Valproic acid

    HDAC inhibitor

    Valproic acid is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
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  7. A15934
    ACY-738

    HDAC6 inhibitor

    ACY-738 is a potent and selective HDAC6 inhibitor with improved brain bioavailability. ACY-738 inhibits HDAC6 with low nanomolar potency and a selectivity of 60- to 1500-fold over class I HDACs.
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  8. A10516
    LAQ824 (NVP-LAQ824, Dacinostat)

    HDAC Inhibitor

    LAQ824 (NVP-LAQ824) is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma.
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  9. A10947
    Trichostatin A (TSA)

    HDAC Inhibitor

    Trichostatin A (TSA) inhibits the HDACs 1, 3, 4, 6 and 10 with IC50 values around 20 nM.
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  10. A10488
    ITF2357 (Givinostat)

    HDAC inhibitor

    ITF2357 (Givinostat) is a HDACs inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities.
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  11. A10830
    SB939 ( Pracinostat )

    HDAC inhibitor

    SB939 is an oral inhibitor of HDAC, selective for class I, II and IV HDACs and displays an IC50 value of 77 nM in an in vitro HDAC1 activity assay.
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  12. A16431
    CAY10603

    HDAC6 inhibitor

    CAY10603 is a potent and selective HDAC6 inhibitor with IC50 of 2 pM, >200-fold selectivity over other HDACs.
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  13. A11042
    Tubastatin A HCl

    HDAC6 inhibitor

    Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold).
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  14. A10518
    LBH589 (Panobinostat)

    HDAC Inhibitor

    LBH589 is a hydroxamic acid and acts as a non-selective HDAC inhibitor with IC5o of HDAC1 to be 0.23 nM.
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  15. A10700
    PCI-24781 (Abexinostat)

    HDAC Inhibitor

    PCI-24781 is a broad-spectrum phenyl hydroxamic acid HDAC inhibitor.
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  16. A15437
    R306465

    HDAC inhibitor

    R306465 is a novel hydroxamate-based histone deacetylase (HDAC) inhibitor with broad-spectrum antitumour activity against solid and haematological malignancies in preclinical models.
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  17. A10586
    MGCD0103 (Mocetinostat)

    HDAC Inhibitor

    MGCD0103 (Mocetinostat) is a benzamide histone deacetylase inhibitor by inhibiting mainly histone deacetylase 1 (HDAC1), but also HDAC2, HDAC3, and HDAC11.
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  18. A10492
    JNJ-26481585 (Quisinostat)

    HDAC inhibitor

    JNJ-26481585 (Quisinostat) is a pan-HDAC inhibitor with marked potency toward HDAC1 (IC(50), 0.16 nmol/L).
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  19. A10979
    Vorinostat (SAHA)

    HDAC inhibitor

    Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.
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  20. A21984
    Sulforaphane

    HDAC inhibitor

    Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
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  21. A10122
    Belinostat (PXD101)

    HDAC inhibitor

    Belinostat (PXD101) is a HDAC inhibitor that inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nM.
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  22. A13218
    RGFP966

    HDAC3 inhibitor

    RGFP966 is an HDAC3 inhibitor with IC50 of 0.08 μM, exhibits > 200-fold selectivity over other HDAC.
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  23. A14128
    TMP 269

    HDAC inhibitor

    TMP 269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
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  24. A11037
    AR-42 (HDAC-42)

    HDAC inhibitor

    AR-42 is a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit.
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  25. A10246
    CUDC-101

    HDAC inhibitor

    CUDC-101 is a novel compound which inhibits multiple targets, which is designed to inhibit HDAC, EGFR and Her2.
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  26. A10337
    Droxinostat

    HDAC inhibitor

    Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 that shows comparable inhibition of HDAC6 and HDAC8 with IC50 = 2.47 and 1.46 μmol/L, respectively.
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  27. A10698
    Parthenolide ((-)-Parthenolide)
    Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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  28. A10764
    Pyroxamide (NSC 696085)

    HDAC Inhibitor

    Pyroxamide (NSC 696085) is a potent inhibitor of affinity-purified HDAC1 and causes the accumulation of acetylated core histones in MEL cells cultured with the agent.
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  29. A10852
    Sodium butyrate

    HDAC inhibitor

    Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs).
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  30. A10855
    Valproic acid sodium salt

    HDAC inhibitor

    Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2.
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  31. A10954
    Tubacin

    HDAC6 inhibitor

    Tubacin (tubulin acetylation inducer) is a highly potent and selective, reversible, cell-permeable HDAC6 inhibitor with an IC50 of 4 nM.
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  32. A22581
    Suberoyl bis-hydroxamic acid

    HDAC1 and HDAC3 inhibitor

    Suberoyl bis-hydroxamic acid (Suberohydroxamic acid; SBHA) is a competitive and cell-permeable HDAC1 and HDAC3 inhibitor with ID50 values of 0.25 μM and 0.30 μM, respectively.
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  33. A24679
    Boc-Lys(Ac)-AMC

    Fluorometric HDAC Substrate

    Boc-Lys(Ac)-AMC is a cell-permeable fluorometric substrate for histone deacetylases (HDACs). When cleaved by HDAC enzymes, it releases a fluorescent signal with excitation and emission maxima at 355 nm and 460 nm, respectively. This compound is valuable for studying HDAC activity in various biological contexts and can be utilized in high-throughput screening assays to evaluate enzyme inhibitors.
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  34. A24799
    VUBI1 analogue-1

    VUBI1 Analogue

    VUBI1 analogue-1 is an analogue of VUBI1, functioning as a selective activator of the SOS1 pathway with a Kd of 44 nM. This compound is valuable for studying SOS1 activation mechanisms and provides a basis for the synthesis of (4S)-PROTAC SOS1 degrader-1. Its applications include investigations into targeted degradation and modulation of cellular pathways involving SOS1, offering insights into cellular signaling and potential therapeutic strategies.
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  35. A24881
    HC-Toxin

    HDAC Inhibitor

    HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression.
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  36. A10926
    Theophylline

    PDE Inhibitor

    Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD).
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  37. A25160
    HDAC3-IN-2

    HDAC3 Inhibitor

    HDAC3-IN-2 is a potent inhibitor of histone deacetylase 3 (HDAC3), with an IC50 value of 14 nM. This pyrazinyl hydrazide compound exhibits cytotoxicity against triple-negative breast cancer cell lines, demonstrating an IC50 of 0.55 μM for 4T1 cells and 0.74 μM for MDA-MB-231 cells. In in vivo studies using tumor-bearing mouse models, HDAC3-IN-2 effectively enhances histone acetylation levels at H3K9, H3K27, and H4K12 while promoting apoptosis through increased caspase-3, caspase-7, and cytochrome c levels, alongside a decrease in proliferation markers such as Bcl-2, CD44, EGFR, and Ki-67.
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  38. A25362
    HDAC1/6-IN-3

    HDAC1/6 Inhibitor

    HDAC1/6-IN-3 is a potent inhibitor of histone deacetylases 1 and 6 (HDAC1 and HDAC6). It demonstrates strong inhibitory activity, with IC50 values of 1.1 nM for HDAC1 and 2.7 nM for HDAC6. This compound effectively induces cell cycle arrest in the G0/G1 phase and promotes both apoptosis and pyroptosis in HepG2 cells. Additionally, HDAC1/6-IN-3 exhibits significant antitumor effects in the HepG2 xenograft model and is valuable for research focused on various types of cancer, including liver, lung, colon, and breast cancers.
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  39. A31141
    HDAC/JAK/BRD4-IN-1

    HDAC/JAK/BRD4 Inhibitor

    HDAC/JAK/BRD4-IN-1 is a potent inhibitor targeting histone deacetylases (HDAC), Janus kinases (JAK), and bromodomain-containing protein 4 (BRD4). This compound demonstrates significant anti-proliferative effects and promotes apoptosis in MDA-MB-231 breast cancer cells. Additionally, HDAC/JAK/BRD4-IN-1 exhibits promising anticancer activity in vivo, making it a valuable tool for research in cancer therapeutics and the study of epigenetic and signaling pathways.
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  40. A31318
    HDAC-IN-53

    HDAC1-3 Inhibitor

    HDAC-IN-53 is a selective inhibitor of histone deacetylases 1-3, demonstrating IC50 values of 47 nM, 125 nM, and 450 nM for HDAC1, HDAC2, and HDAC3, respectively. This compound exhibits minimal off-target effects, as it does not inhibit class II HDACs (IC50 > 10 μM). HDAC-IN-53 promotes caspase-dependent apoptosis and has been shown to inhibit the growth of human tumor xenografts in nude mice, as well as murine tumors in immune-competent mice bearing MC38 colon cancer. It serves as a valuable tool for studying cancer biology and potential therapeutic strategies targeting HDAC pathways.
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  41. A31356
    QTX125 TFA

    HDAC6 Inhibitor

    QTX125 TFA is a potent and highly selective inhibitor of Histone Deacetylase 6 (HDAC6). This compound demonstrates exceptional selectivity for HDAC6 over other isoforms, making it a valuable tool for studying the role of HDAC6 in various biological processes. QTX125 TFA has shown promising antitumor effects, indicating its potential for use in cancer research and therapeutic applications targeting HDAC6-related pathways.
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  42. A31382
    CRA-026440 hydrochloride

    HDAC Inhibitor

    CRA-026440 hydrochloride is a potent, broad-spectrum histone deacetylase (HDAC) inhibitor, exhibiting Ki values against recombinant HDAC isoenzymes of 4 nM for HDAC1, 14 nM for HDAC2, 11 nM for HDAC3, 15 nM for HDAC6, 7 nM for HDAC8, and 20 nM for HDAC10. This compound demonstrates significant antitumor and antiangiogenic activities, making it relevant for studies in cancer biology. Additionally, CRA-026440 hydrochloride possesses an alkyne functional group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating its use in click chemistry applications for bioconjugation studies.
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  43. A31534
    HDAC1/2 and CDK2-IN-1

    HDAC1/2 and CDK2 Inhibitor

    HDAC1/2 and CDK2-IN-1 is a dual inhibitor targeting HDAC1, HDAC2, and CDK2, with IC50 values of 70.7 μM, 23.1 μM, and 0.80 μM, respectively. This compound effectively disrupts the cell cycle and promotes apoptosis in tumor cells, demonstrating significant in vivo antitumor activity. It is suitable for research applications focused on cancer biology and therapeutic interventions targeting histone deacetylases and cyclin-dependent kinases.
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  44. A31540
    Pracinostat dihydrochloride

    HDAC/MBLAC2 Inhibitor

    Pracinostat dihydrochloride is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values in the range of 40-140 nM, making it a valuable tool in cancer research. In addition, it effectively inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) with an EC50 below 10 nM, highlighting its potential use in studies related to epigenetic regulation and resistance mechanisms in cancer therapies.
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  45. A31676
    HDAC-IN-73

    HDAC Inhibitor

    HDAC-IN-73 is a potent histone deacetylase (HDAC) inhibitor targeting HDAC1 and HDAC6, with IC50 values of 0.17 µM and 0.49 µM, respectively. Its enhanced activity against HDAC6 demonstrates a nine-fold greater potency compared to PsA, making it a valuable compound in the field of cancer research. HDAC-IN-73 exhibits significant antiproliferative effects, induces apoptosis, and triggers G2/M cell cycle arrest, positioning it as a promising candidate for investigating therapies in colon cancer and other malignancies.
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  46. A31685
    HDAC-IN-96

    HDAC Inhibitor

    HDAC-IN-96 is a selective inhibitor of histone deacetylases 1 and 2 (HDAC1/2), exhibiting IC50 values of 457.1 nM and 433.7 nM, respectively. This compound demonstrates significant cytotoxicity against various hematological tumor cell lines, including RS4;11, K562, RPMI-8226, and U266, with IC50 values between 2.11 and 5.35 μM. HDAC-IN-96 has been shown to induce apoptosis and cause S phase arrest in cancer cells, making it a valuable tool for research in hematological malignancies such as acute lymphoblastic leukemia.
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  47. A31695
    Aurora kinase/HDAC-IN-1

    Aurora A/Aurora B/HDAC1/HDAC2 Inhibitor

    Aurora kinase/HDAC-IN-1 is a potent dual inhibitor targeting Aurora A, Aurora B, HDAC1, and HDAC2. This compound promotes histone H3 acetylation, inhibits Aurora A phosphorylation and downstream signaling, and induces apoptosis through G2/M cell-cycle arrest. It demonstrates significant antiproliferative activity in colorectal cancer cells, with an IC50 of 30.2 nM in HCT-116 cells, and effectively suppresses tumor growth in HCT-116 colorectal cancer xenograft mouse models. This reagent is valuable for research in cancer biology and therapeutic application development.
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  48. A31716
    HDAC1/CDK7-IN-1

    HDAC1/CDK7 Inhibitor

    HDAC1/CDK7-IN-1 is a dual inhibitor targeting HDAC1 and CDK7, exhibiting IC50 values of 893 nM and 248 nM, respectively. This compound effectively inhibits the proliferation of cancer cell lines, including MDA-MB-231, MCF-7, A549, and HCT-116. Additionally, HDAC1/CDK7-IN-1 induces cell cycle arrest and apoptosis specifically in HCT-116 cells, while also disrupting their migratory capacity. These properties make it a valuable tool for cancer research, particularly in exploring therapeutic strategies that target epigenetic regulation and cell cycle dynamics.
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  49. A31720
    WMJ-J-09

    HDAC Inhibitor

    WMJ-J-09 is a potent HDAC inhibitor with sub-nanomolar activity, exhibiting IC50 values of 7.5 nM against HDAC1 and 3.9 nM against HDAC6, along with notable activity towards HDAC2, HDAC3, and HDAC8. This compound effectively disrupts the cell cycle and promotes apoptosis in cancer cells through the LKB1-AMPK-p38MAPK-p63-survivin signaling pathway. By inhibiting HDAC enzyme activity, WMJ-J-09 leads to the acetylation of critical proteins, thus contributing to the regulation of cell death in cancer models, such as HCT116 and FaDu cells.
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  50. A31730
    TH-6

    HDAC Inhibitor

    TH-6 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.115 µM for HDAC1, 0.135 µM for HDAC2, 0.242 µM for HDAC3, 0.138 µM for HDAC6, and 2.120 µM for HDAC8. This compound effectively inhibits cell migration and invasion while promoting apoptosis and inducing cell cycle arrest in the G2/M phase. TH-6 exhibits significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic studies.
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