HDAC1

Cat. No.

A26331

CAS No.

2756809-34-2

HDAC-IN-30

HDAC-IN-30 is a potent multi-target histone deacetylase (HDAC) inhibitor, demonstrating strong inhibition of HDAC1 (IC50 = 13.4 nM), HDAC2 (IC50 = 28.0 nM), HDAC3 (IC50 = 9.18 nM), HDAC6 (IC50 = 42.7 nM), and HDAC8 (IC50 = 131 nM). This compound exhibits significant antitumor activity, making it a valuable tool for cancer research and potential therapeutic applications in oncology. Its ability to modulate gene expression through HDAC inhibition positions HDAC-IN-30 as an important reagent in epigenetic studies and cancer treatment research.

Cat. No.

A26332

CAS No.

2599838-15-8

HDAC/CK2-IN-1

HDAC/CK2-IN-1 is an inhibitor targeting histone deacetylases HDAC1 and HDAC6, with IC50 values of 1.46 μM and 0.66 μM, respectively, as well as casein kinase 2 (CK2) with an IC50 of 3.67 μM. This compound demonstrates significant antiproliferative effects on various cancer cell lines, including Jurkat, MCF-7, HCT-116, and HL-60. It serves as an important research tool for studying the roles of histone modifications and CK2 in tumor biology and could have potential implications in the development of cancer therapeutics.

Cat. No.

A26336

CAS No.

2767560-94-9

A2AAR/HDAC-IN-2

A2AAR/HDAC-IN-2 is a potent dual inhibitor targeting the adenosine A2A receptor (A2AAR) and histone deacetylase 1 (HDAC1). It demonstrates a strong binding affinity for A2AAR with a Ki value of 10.3 nM and exhibits significant inhibitory activity against HDAC1 with an IC50 of 18.5 nM. This compound is applicable in cancer research, particularly in studies exploring antitumor mechanisms and therapeutic efficacy.

Cat. No.

A26339

CAS No.

2766688-19-9

HDAC-IN-33

HDAC-IN-33 is a potent inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 24 nM, 46 nM, and 47 nM for HDAC1, HDAC2, and HDAC6, respectively. This compound demonstrates significant antiproliferative activity against various tumor cell lines, contributing to its potential as an anticancer agent. Furthermore, HDAC-IN-33 has shown promising antitumor efficacy in vivo, promoting antitumor immune responses that may enhance its therapeutic potential in cancer research applications.

Cat. No.

A26340

CAS No.

3037978-19-8

HDAC6-IN-43

HDAC6-IN-43 is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 value of 11 nM, demonstrating potent activity against other HDACs, including HDAC1 and HDAC2 (IC50 < 150 nM). By inhibiting HDAC6, this compound contributes to the modulation of acetylation processes, which are critical for cellular functions. HDAC6-IN-43 is relevant for research applications in autosomal dominant polycystic kidney disease (ADPKD) and other conditions involving dysregulated histone modification.

Cat. No.

A26341

CAS No.

244289-53-0

HDAC1/3-IN-1

HDAC1/3-IN-1 is a selective inhibitor targeting histone deacetylases HDAC1 and HDAC3, exhibiting IC50 values of 256 nM and 340.3 nM, respectively. This compound has been shown to increase the SubG1 cell population and promote apoptosis in glioma cells and glioblastoma stem cells. HDAC1/3-IN-1 is ideal for research applications focused on investigating glioblastoma and exploring therapeutic strategies for glioma-related disorders.

Cat. No.

A26342

CAS No.

1083078-98-1

Quisinostat hydrochloride

Synonyms: JNJ26481585 hydrochloride

Quisinostat hydrochloride is a potent pan-HDAC inhibitor, exhibiting IC50 values between 0.11 nM and 0.64 nM for multiple HDAC targets including HDAC1, HDAC2, HDAC4, HDAC10, and HDAC11. This compound demonstrates significant antitumoral activity across various cancer models. Additionally, Quisinostat hydrochloride has been shown to induce autophagy in neuroblastoma cells, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A26343

CAS No.

2222756-46-7

Rodin-A

Rodin-A is a selective histone deacetylase (HDAC) and CoREST complex inhibitor, demonstrating an IC50 of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. This orally active compound enhances histone H3K9 acetylation and upregulates neuron-related gene expression, which promotes dendritic spine density and the colocalization of synaptic proteins such as SV2A and PSD95. Additionally, Rodin-A improves hippocampal long-term potentiation, indicating its potential for neuroprotective and restorative applications in research on neurodegenerative diseases, particularly Alzheimer’s disease.

Cat. No.

A26347

CAS No.

3056145-98-0

LSD1/HDAC-IN-1

LSD1/HDAC-IN-1 is a potent inhibitor of histone deacetylases (HDACs) and lysine-specific demethylase 1 (LSD1), demonstrating impressive inhibitory activity with IC50 values of 0.125 nM for HDAC1, 0.373 nM for HDAC2, 0.0118 nM for HDAC6, 0.103 nM for HDAC8, and 0.571 μM for LSD1. This compound is significant in cancer research, as it influences gene expression and histone modification, making it a valuable tool for studies addressing epigenetic regulation and potential therapeutic interventions.

Cat. No.

A26348

CAS No.

2669785-76-4

JPS014

JPS014 is a benzamide-based HDAC degrader designed to engage the Von Hippel-Lindau (VHL) E3 ligase for targeted proteolysis. It effectively degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression profiles and promoting apoptotic pathways in HCT116 cancer cells. This compound is particularly useful for studying the role of HDAC inhibition in cancer biology and elucidating mechanisms of resistance to therapies.

Cat. No.

A26349

CAS No.

2127411-50-9

M122

M122 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, demonstrating IC50 values of 0.48 μM and 0.47 μM, respectively. This compound exhibits significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate gene expression through epigenetic mechanisms positions M122 as a potential candidate for studies in cancer therapeutics and epigenetic regulation.

Cat. No.

A26354

CAS No.

2127411-61-2

M133

M133 is a selective inhibitor of HDAC1 and HDAC2, demonstrating potent antiproliferative activity against various human tumor cell lines with IC50 values ranging from 0.75 to 1.94 μM. This compound serves as a valuable tool for cancer research, facilitating the investigation of histone deacetylase activity and its implications in tumor biology.

Cat. No.

A26360

CAS No.

4312-91-8

Butyrylhydroxamic acid

Synonyms: N-Hydroxybutanamide

Butyrylhydroxamic acid is a selective inhibitor of histone deacetylase (HDAC), modulating gene expression by preventing histone deacetylation. Its biological activity has been shown to enhance cognitive functions in rodent models, suggesting potential applications in memory enhancement and mood stabilization. Additionally, it is being explored in research related to β-chain hemoglobinopathies, providing valuable insights into therapeutic strategies for related disorders.

Cat. No.

A26364

CAS No.

2898381-63-8

HDAC/NAMPT-IN-1

HDAC/NAMPT-IN-1 is a potent dual inhibitor of histone deacetylases (HDAC) and nicotinamide adenine dinucleotide (NAD+) biosynthesis enzyme NAMPT, exhibiting IC50 values ranging from 0.72 to 37081 nM for HDAC and 1618 nM for NAMPT. This compound demonstrates significant potential in modulating cellular acetylation levels and metabolic processes associated with cancer and neurodegenerative diseases. Its application in research can facilitate studies on epigenetic regulation and NAD+ metabolism, contributing to a deeper understanding of cellular mechanisms and therapeutic strategies.

Cat. No.

A26367

CAS No.

2408123-36-2

HDAC-IN-38

HDAC-IN-38 is a potent inhibitor of histone deacetylases (HDACs), targeting HDAC1, 2, 3, 5, 6, and 8 with micromolar inhibitory activity. This compound has been shown to enhance cerebral blood flow, mitigate cognitive impairment, and reduce hippocampal atrophy. Additionally, HDAC-IN-38 increases histone acetylation levels, specifically H3K14 and H4K5, making it a valuable tool for studying the epigenetic regulation of gene expression and its implications in neurodegenerative disorders.

Cat. No.

A26370

CAS No.

3032392-39-2

GK444

GK444 is an inhibitor of histone deacetylases HDAC1 and HDAC2, with IC50 values of 100 nM and 92 nM, respectively. This compound demonstrates significant biological activity by inhibiting Caco-2 cell proliferation, showcasing an IC50 of 4.1 μM. Additionally, GK444 effectively reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts and has been shown to inhibit Bleomycin-induced lung fibrosis in murine models. Its applications extend to research in cancer, fibrosis, and other HDAC-related pathways.

Cat. No.

A26371

CAS No.

1809163-24-3

HDAC-IN-43

HDAC-IN-43 is a potent inhibitor of histone deacetylases HDAC1, HDAC3, and HDAC6, exhibiting IC50 values of 82 nM, 45 nM, and 24 nM, respectively. Additionally, it acts as a weak inhibitor of PI3K and mTOR, with IC50 values of 3.6 μM and 3.7 μM. This compound demonstrates significant anti-proliferative activity, making it a valuable tool for research on cancer and epigenetic regulation.

Cat. No.

A26375

CAS No.

3006905-22-9

PI3K/HDAC-IN-3

PI3K/HDAC-IN-3 is a dual inhibitor targeting PI3K and HDAC, with IC50 values of 0.23 nM for PI3Kα and 172 nM for HDAC1. It effectively suppresses AKT phosphorylation while enhancing H3 acetylation in MV4-11 cells. Additionally, PI3K/HDAC-IN-3 demonstrates notable anticancer efficacy in a dose-dependent manner within an MV4-11 xenograft model, making it a valuable tool for studying cancer biology and potential therapeutic interventions.

Cat. No.

A26376

CAS No.

2548725-57-9

DNMT/HDAC-IN-2

DNMT/HDAC-IN-2 is a dual inhibitor of DNA methyltransferase (DNMT) and histone deacetylases (HDAC), exhibiting IC50 values of 365 nM for DNMT1, 0.2 nM for HDAC1, and 8.91 nM for HDAC6. This compound effectively inhibits the proliferation of breast cancer cells and demonstrates significant anti-tumor activity in xenograft and transgenic mouse models of breast cancer. DNMT/HDAC-IN-2 serves as a valuable tool for investigating epigenetic modification in breast cancer research.

Cat. No.

A26382

CAS No.

2759855-37-1

HDAC1/MAO-B-IN-1

HDAC1/MAO-B-IN-1 is a selective inhibitor targeting both HDAC1 and MAO-B, exhibiting IC50 values of 21.4 nM and 99.0 nM, respectively. This compound effectively crosses the blood-brain barrier, making it a valuable tool for studying neurological disorders. Its potential applications include research into Alzheimer's disease and related pathologies, facilitating the exploration of epigenetic modifications and monoamine metabolism in the brain.

Cat. No.

A26384

CAS No.

2490309-83-4

HDAC-IN-41

HDAC-IN-41 is a selective class I histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 0.62 µM for HDAC1, 1.46 µM for HDAC2, and 0.62 µM for HDAC3. This compound is orally active and demonstrates potential in modulating gene expression through HDAC inhibition. Applications in research include studies on cancer, neurodegenerative diseases, and epigenetic regulation. Notably, HDAC-IN-41 does not exhibit NO releasing activity.

Cat. No.

A26388

CAS No.

3032392-65-4

GK718

GK718 is a potent inhibitor of histone deacetylases 1 and 3 (HDAC1/3), exhibiting IC50 values of 259 nM and 139 nM, respectively. This compound effectively increases the levels of acetylated histone H3 in cells, indicating its potential for altering epigenetic regulation. Additionally, GK718 has demonstrated efficacy in inhibiting Bleomycin-induced pulmonary fibrosis in murine models, making it relevant for research into fibrotic diseases and epigenetic modifications.

Cat. No.

A26393

CAS No.

2763368-90-5

HDAC3-IN-8

HDAC3-IN-8 is a selective inhibitor targeting histone deacetylase 3 (HDAC3) with an IC50 of 0.38 nM, along with notable inhibition of HDAC1 and HDAC2 at 3.52 nM and 15.14 nM, respectively. This compound demonstrates high selectivity for HDAC3 and modulates histone deacetylase activity, making it a valuable tool for epigenetic research. HDAC3-IN-8 is particularly applicable in studies focused on acute myeloid leukemia (AML) and can be utilized in the development of HDAC3-targeted PROTAC degraders.

Cat. No.

A26394

CAS No.

651293-70-8

AW01178

AW01178 is a Class I histone deacetylase (HDAC) inhibitor that plays a critical role in regulating gene expression. This compound has been shown to induce the upregulation of E-cadherin at both the mRNA and protein levels, effectively inhibiting the epithelial-mesenchymal transition (EMT) in breast cancer cells. AW01178 is a valuable tool for researchers investigating the mechanisms of cancer progression and potential therapeutic strategies targeting HDAC activity.

Cat. No.

A26398

CAS No.

2411379-14-9

HDAC/Top-IN-1

HDAC/Top-IN-1 is a potent dual inhibitor targeting histone deacetylases (HDACs) and topoisomerases, with IC50 values of 0.036 μM, 0.14 μM, 0.059 μM, 0.089 μM, and 9.8 μM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. This compound effectively induces apoptosis and S phase cell-cycle arrest in HEL cells, demonstrating its antiproliferative properties. Additionally, HDAC/Top-IN-1 exhibits significant in vivo antitumor efficacy, making it a valuable tool for cancer research applications.