HDAC1 | Adooq Bioscience

Cat. No.: A26489

CAS No.: 2814571-89-4

HDAC-IN-56

HDAC-IN-56 is a potent, orally active inhibitor of class I histone deacetylases (HDACs), demonstrating IC50 values of 56.0 ± 6.0 nM for HDAC1, 90.0 ± 5.9 nM for HDAC2, and 422.2 ± 105.1 nM for HDAC3, with minimal activity against HDAC4-11. This compound effectively increases intracellular levels of acetylated histone H3 and P21, leading to G1 cell cycle arrest and apoptosis in tumor cells. HDAC-IN-56 is utilized in cancer research to investigate its therapeutic potential and mechanisms involving HDAC inhibition.

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Cat. No.: A26490

CAS No.: 2420562-65-6

IHCH-3064

IHCH-3064 is a dual-target compound that inhibits the Adenosine A2A Receptor and histone deacetylase (HDAC). It demonstrates potent binding affinity for the A2A receptor (Ki = 2.2 nM) and selectively inhibits HDAC1 with an IC50 of 80.2 nM. This compound exhibits significant antiproliferative activity against various tumor cell lines in vitro, making it a valuable tool for tumor immunotherapy research applications.

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Cat. No.: A26493

CAS No.: 3066143-73-2

HDAC1-IN-8

HDAC1-IN-8 is a selective inhibitor of histone deacetylase 1 (HDAC1) with an IC50 of 11.94 µM. It exhibits significant antiproliferative activity and has been shown to induce cell cycle arrest at both G1 and G2/M phases. Additionally, HDAC1-IN-8 promotes autophagy and demonstrates anticancer potential, making it a valuable tool for research in lung cancer and other malignancies.

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Cat. No.: A26494

CAS No.: 300399-36-4

HDAC1 activator-1

HDAC1 activator-1 is a selective activator of histone deacetylase 1 (HDAC1), demonstrating oral bioavailability and minimal cross-reactivity with other HDAC family members. This compound exhibits neuroprotective properties, enhancing cognitive and motor functions by mitigating neuronal loss and gliosis. HDAC1 activator-1 effectively activates HDAC1 in SH-SY5Y neuroblastoma cells, influencing cell cycle regulation and DNA damage responses. It is applicable in research investigating TDP-43 proteinopathy-related neurodegenerative disorders, including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-associated neurological injuries.

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Cat. No.: A26500

CAS No.: 2421122-61-2

HDAC-IN-45

HDAC-IN-45 is a small molecule inhibitor targeting histone deacetylases (HDACs), specifically demonstrating significant inhibition of HDAC1, HDAC2, and HDAC3 with IC50 values of 0.108 µM, 0.585 µM, and 0.563 µM, respectively. This compound exhibits pronounced anticancer activity and forms a hydrogen bond with the Y303 residue, which may contribute to its mechanism of action. HDAC-IN-45 is valuable for cancer research, particularly in studies focused on epigenetic regulation and therapeutic interventions in tumorigenesis.

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Cat. No.: A26504

CAS No.: 2919691-32-8

HDAC2-IN-1

HDAC2-IN-1 is a competitive inhibitor of histone deacetylase 2 (HDAC2), demonstrating an IC50 of 0.5 μM. This orally active compound exhibits additional inhibitory effects on HDAC1 and HDAC8, with IC50 values of 1.61 μM and 0.98 μM, respectively. Its ability to penetrate the blood-brain barrier positions HDAC2-IN-1 as a valuable tool for investigating the role of HDACs in neurodegenerative diseases and other neurological disorders.

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Cat. No.: A26510

CAS No.: 2339867-53-5

PHD2/HDACs-IN-1

PHD2/HDACs-IN-1 is a dual inhibitor targeting both PHD2 and various HDACs, demonstrating potent inhibitory activity with IC50 values of 1.15 μM for PHD2, 19.75 μM for HDAC1, 26.60 μM for HDAC2, and 15.98 μM for HDAC6. This compound showcases low toxicity and exhibits renoprotective effects, making it suitable for research related to cisplatin-induced acute kidney injury (AKI). Its ability to modulate epigenetic regulation and hypoxic signaling pathways positions it as a valuable tool in exploring the underlying mechanisms of renal stress responses.

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Cat. No.: A26516

CAS No.: 2482998-39-8

HDAC1-IN-4

HDAC1-IN-4 is a potent inhibitor of Plasmodium falciparum histone deacetylase 1 (PfHDAC1), demonstrating significant antimalarial activity with an IC50 of less than 5 nM. This compound exhibits a favorable safety profile with reduced cytotoxicity. HDAC1-IN-4 serves as a valuable tool for investigating the role of histone deacetylases in malaria research and may provide insights for novel therapeutic strategies against Plasmodium falciparum infections.

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Cat. No.: A26517

CAS No.: 2361418-65-5

PI3K/HDAC-IN-2

PI3K/HDAC-IN-2 is a potent dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), demonstrating IC50 values of 226 nM for PI3Kα, 279 nM for PI3Kβ, 467 nM for PI3Kγ, and 29 nM for PI3Kδ. It also exhibits selective inhibition with IC50 values of 1.3 nM for HDAC1, 3.4 nM for HDAC2, 972 nM for HDAC4, 17 nM for HDAC6, and 12 nM for HDAC8. Due to its significant anticancer properties, PI3K/HDAC-IN-2 is valuable for research applications in cancer biology and therapeutic development.

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Cat. No.: A26520

CAS No.: 2815286-02-1

mTOR/HDAC-IN-1

mTOR/HDAC-IN-1 is a dual inhibitor targeting mTOR and HDAC, exhibiting IC50 values of 0.49 nM and 0.91 nM for mTOR and HDAC1, respectively. This compound demonstrates significant anti-cancer activity, making it a valuable tool for research in cancer therapeutics and signaling pathways. Its selective inhibition profile offers potential for elucidating the roles of mTOR and HDAC in tumorigenesis and for developing novel cancer treatment strategies.

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Cat. No.: A26532

CAS No.: 2095619-17-1

DNMT/HDAC-IN-1

DNMT/HDAC-IN-1 is a dual inhibitor targeting DNA methyltransferases (DNMT) and histone deacetylases (HDACs), demonstrating IC50 values of 56.84 nM for HDAC1 and 17.39 nM for HDAC6. This compound induces apoptosis in tumor cells and is valuable for cancer research applications, providing insights into the mechanisms of epigenetic regulation in malignancies. Its role in modulating both DNMT and HDAC activities makes it a significant tool for investigating therapeutic strategies in oncology.

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Cat. No.: A26533

CAS No.: 794552-20-8

HDAC1-IN-7

HDAC1-IN-7 is a potent inhibitor of histone deacetylase 1 (HDAC1), exhibiting an IC50 of 0.957 mM. This compound serves as a valuable tool for investigating the role of HDAC1 in various biological processes, including gene expression regulation and cellular differentiation. Its application is relevant in studies of cancer biology and neurodegenerative disorders, where modulation of HDAC1 activity may provide insights into therapeutic strategies.

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5 mg

$295.00

10 mg

$485.00

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Cat. No.: A26537

CAS No.: 2978763-95-8

HD-TAC7

HD-TAC7 is a highly effective PROTAC HDAC degrader, specifically targeting histone deacetylases HDAC1, HDAC2, and HDAC3 with IC50 values of 3.6 μM, 4.2 μM, and 1.1 μM, respectively. This compound has demonstrated the ability to reduce NF-κB p65 levels in RAW 264.7 macrophages. HD-TAC7 is suitable for research applications focused on inflammatory diseases, including asthma and chronic obstructive pulmonary disease (COPD).

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1 mg

$160.00

5 mg

$375.00

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Cat. No.: A26541

CAS No.: 3023019-99-7

HDAC6-IN-3

HDAC6-IN-3 is a potent inhibitor of histone deacetylase 6 (HDAC6), with an IC50 ranging from 0.02 to 1.54 μM for various HDAC isoforms, including HDAC1, HDAC2, HDAC3, and HDAC8. Additionally, it exhibits significant inhibitory activity against monoamine oxidase A (MAO-A) with an IC50 of 0.79 μM and lysine-specific demethylase 1 (LSD1). This compound serves as a valuable tool for research applications in cancer biology and epigenetics and is equipped with an alkyne functionality, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc).

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5 mg

$420.00

10 mg

$695.00

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Cat. No.: A26547

CAS No.: 1628784-53-1

BG48

BG48 is a potent histone deacetylase (HDAC) inhibitor that selectively targets HDAC1 and HDAC2. By inhibiting the enzymatic activity of these enzymes, BG48 modulates gene expression and can influence cellular processes such as differentiation, proliferation, and apoptosis. This compound is valuable for research applications in cancer biology, neurodegenerative diseases, and epigenetic studies.

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5 mg

$305.00

10 mg

$525.00

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Cat. No.: A26548

CAS No.: 1929583-17-4

Purinostat

Purinostat is a selective inhibitor of histone deacetylases (HDAC) I and IIb, exhibiting potent anti-leukemic activity. It effectively reduces the survival of Philadelphia chromosome-positive leukemic cells and CD34+ leukemic progenitors from chronic myeloid leukemia patients. By targeting HDAC I/IIb, Purinostat disrupts critical pathways for leukemic stem cell survival, influencing factors such as c-Myc, β-Catenin, E2F, Ezh2, Alox5, and mTOR. Additionally, Purinostat enhances glutamate metabolism in leukemic stem cells by upregulating GLS1.

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5 mg

$460.00

10 mg

$755.00

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Cat. No.: A26550

CAS No.: 2669785-85-5

JPS036

JPS036 is a benzamide-based HDAC degrader that operates through the Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC) mechanism. This compound selectively degrades class I histone deacetylases (HDAC1 and HDAC2), demonstrating significant biological activity by promoting the expression of differentially expressed genes and enhancing apoptosis in HCT116 cells. JPS036 serves as a valuable research tool for studying the roles of HDACs in cellular processes and disease models.

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Cat. No.: A26563

CAS No.: 1628784-54-2

BG47

BG47 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, functioning as an optoepigenetic probe. Upon light-induced trans-to-cis isomerization, BG47 competitively inhibits the deacetylase activity of its targets, resulting in increased acetylation of Histone H3K9. This compound is relevant for research applications in neurological diseases, providing insights into epigenetic regulation and its implications in various disorders.

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Cat. No.: A29074

CAS No.: 1326750-61-1

MHY219

MHY219 is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 0.276 μM, effectively inhibiting total HDAC enzyme activity. This compound promotes histone H3 and H4 hyperacetylation, leading to cell cycle arrest, apoptosis, and reduced proliferation in cancer cells. Additionally, MHY219 enhances cleavage of PARP, Bax, and cytochrome c levels, while upregulating androgen receptor expression and downregulating Bcl-2 expression. It serves as a valuable research tool for studying prostate cancer mechanisms and potential therapeutic strategies.

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Cat. No.: A31042

CAS No.: 3069831-25-7

HDAC-IN-27 dihydrochloride

HDAC-IN-27 dihydrochloride is a potent inhibitor of class I histone deacetylases (HDAC1-3) with IC50 values ranging from 0.43 to 3.01 nM. This compound displays significant antitumor activity both in vitro and in vivo, particularly against acute myeloid leukemia (AML) cell lines, through mechanisms that include apoptosis induction and increased histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 dihydrochloride is an important tool for investigating the roles of HDACs in cancer biology, specifically within the context of AML research.

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Cat. No.: A31318

CAS No.: 2921948-27-6

HDAC-IN-53

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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1 mg

$385.00

5 mg

$985.00

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Cat. No.: A31382

CAS No.: 847459-98-7

CRA-026440 hydrochloride

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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1 mg

$95.00

5 mg

$235.00

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Cat. No.: A31540

CAS No.: 929016-98-8

Pracinostat dihydrochloride

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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Cat. No.: A31676

CAS No.: 2323571-16-8

HDAC-IN-73

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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Cat. No.: A31685

CAS No.: 3055552-13-8

HDAC-IN-96

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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