HDAC1

Cat. No.

A26407

CAS No.

2007971-51-7

CM-414

CM-414 is a potent dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDACs), exhibiting IC50 values of 60 nM for PDE5 and ranging from 91 nM to 490 nM for various HDAC isoforms, including HDAC6 and HDAC1. This compound effectively reduces levels of amyloid-beta (Aβ) and phosphorylated tau (pTau) in Tg2576 mouse models, making it a valuable tool for Alzheimer's disease research. Its ability to penetrate the blood-brain barrier enhances its potential for studying neurodegenerative disorders and therapeutic interventions.

Cat. No.

A26410

CAS No.

2421119-78-8

IOR-160

IOR-160 is a dual inhibitor targeting casein kinase 2 (CK2) and histone deacetylases (HDACs). It showcases high selectivity for CK2, with an IC50 of 1.7 nM, and demonstrates broad inhibitory effects on HDACs 1, 2, 3, and 6, with IC50 values of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively. Through the inhibition of AKT phosphorylation and the enhancement of acetylated α-tubulin levels, IOR-160 effectively modulates critical cellular signaling pathways. This compound is particularly relevant in research focused on triple-negative breast cancer, where it has been shown to inhibit tumor growth and reduce tumor burden.

Cat. No.

A26412

CAS No.

1788896-33-2

NL-103

NL-103 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 21.3 nM, 57 nM, 74 nM, and 680 nM for HDAC1, HDAC2, HDAC3, and HDAC6, respectively. This compound also targets the Hedgehog signaling pathway, leading to the downregulation of Gli2 expression. NL-103 is primarily utilized in cancer research, providing valuable insights into HDAC regulation and its role in tumor biology.

Cat. No.

A26416

CAS No.

2767560-51-8

A2AAR/HDAC-IN-1

A2AAR/HDAC-IN-1 is a potent dual inhibitor targeting the A2A adenosine receptor (A2AAR) and histone deacetylase 1 (HDAC1), with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. This compound demonstrates significant anticancer activity, making it a valuable reagent for research in cancer therapeutics and epigenetic modulation. Its oral bioavailability enhances its utility in in vivo studies, facilitating investigations into the mechanisms underlying tumor growth and proliferation.

Cat. No.

A26428

CAS No.

1793059-58-1

Tinostamustine hydrochloride

Synonyms: EDO-S101 hydrochloride; NL-101 hydrochloride

Tinostamustine hydrochloride is an HDAC inhibitor that exhibits potent anti-multiple myeloma activity. This compound promotes CD38 expression and enhances the acetylation of histone H3, which increases the sensitivity of tumor cells to the anti-CD38 monoclonal antibody daratumumab. Additionally, Tinostamustine hydrochloride elevates the expression of MICA and MICB, thereby activating natural killer (NK) cells. Research indicates that this compound can significantly delay tumor growth and improve survival rates in murine models.

Cat. No.

A26432

CAS No.

3031784-60-5

G4/HDAC-IN-1

G4/HDAC-IN-1 is a dual-targeting compound that inhibits histone deacetylase (HDAC) activity and promotes the formation of G-quadruplex (G4) structures. With an IC50 value of 1.1 μM, this reagent effectively impedes the proliferation of triple-negative breast cancer (TNBC) cells and suppresses tumor growth in TNBC xenograft models. G4/HDAC-IN-1 is highly relevant for research into cancer biology and potential therapeutic strategies.

Cat. No.

A26434

CAS No.

1132667-11-8

Largazole thiol

Largazole thiol is a potent and selective class I histone deacetylase (HDAC) inhibitor that effectively penetrates the blood-brain barrier. This compound exhibits significant antitumor and neuroprotective activities, making it a valuable tool for studying various cancer models, specifically glioblastoma. Its inhibition of HDAC activity may provide insights into therapeutic strategies for neurodegenerative diseases and cancer treatment.

Cat. No.

A26440

CAS No.

1009815-87-5

Largazole

Synonyms: (+)-Largazole

Largazole is a potent and selective Class I HDAC inhibitor, primarily targeting HDAC2 with an IC50 of 0.07 nM. Isolated from marine cyanobacteria, Largazole demonstrates significant antitumor activity against glioblastoma cell lines, including SF-268, SF-295, and SH-SY5Y, with IC50 values ranging from 62 to 102 nM. In addition to its antitumor properties, Largazole enhances the expression of key neuroprotective factors such as brain-derived neurotrophic factor (BDNF) and the transcription factor Pax6, making it a valuable reagent for research in glioblastoma and Alzheimer's disease.

Cat. No.

A26443

CAS No.

2482998-35-4

HDAC1-IN-3

HDAC1-IN-3 is a selective inhibitor of Histone Deacetylase 1 (HDAC1), demonstrating significant antimalarial activity against both wild-type and multidrug-resistant strains of parasites. This compound effectively exhibits a robust in vivo efficacy, resulting in notable parasiticidal effects across all developmental stages of malaria parasites. Its mechanism of action supports further exploration in antimalarial research and potential therapeutic development.

Cat. No.

A26444

CAS No.

1624792-70-6

CM-545

CM-545 is a dual inhibitor targeting both histone deacetylases (HDACs) and phosphodiesterase 5 (PDE5). With pIC50 values of 7.47 for PDE5, 6.65 for HDAC1, 6.14 for HDAC2, 6.55 for HDAC3, and 6.84 for HDAC6, CM-545 demonstrates potent inhibitory activity. This compound has applications in cancer research and therapeutic interventions related to neurodegenerative diseases and cardiovascular conditions, owing to its modulation of histone acetylation and cyclic nucleotide signaling pathways.

Cat. No.

A26445

CAS No.

849233-98-3

HDAC1-IN-10

HDAC1-IN-10 is a selective inhibitor targeting HDAC1 and HDAC2, exhibiting potent activity with IC50 values of 6 nM and 190 nM, respectively, while showing minimal activity against HDAC3-8 (IC50 > 50 μM). This compound demonstrates efficacy in inhibiting tumor growth in HCT-116 colon cancer xenograft models, making it a valuable tool for studying the role of histone deacetylases in colon cancer research. It serves as a potential lead for therapeutic strategies aimed at HDAC-related malignancies.

Cat. No.

A26447

CAS No.

2766688-17-7

HDAC-IN-32

HDAC-IN-32 is a selective histone deacetylase (HDAC) inhibitor, demonstrating IC50 values of 5.2 nM, 11 nM, and 28 nM for HDAC1, HDAC2, and HDAC6, respectively. This compound exhibits significant antiproliferative effects against various tumor cell lines and enhances antitumor immunity in vivo. HDAC-IN-32 is valuable for research applications aimed at understanding the role of HDACs in cancer biology and developing new therapeutic strategies.

Cat. No.

A26448

CAS No.

2075787-77-6

HDAC-IN-52

HDAC-IN-52 is a pyridine-based inhibitor targeting histone deacetylases (HDACs) with IC50 values of 0.189 μM for HDAC1, 0.227 μM for HDAC2, 0.440 μM for HDAC3, and 0.446 μM for HDAC10. This compound exhibits potent HDAC inhibition, making it a valuable tool for investigating epigenetic regulation in cancer research. Its application extends to the study of cell differentiation, apoptosis, and potential therapeutic strategies in oncology.

Cat. No.

A26449

CAS No.

2944087-54-9

CDK/HDAC-IN-3

CDK/HDAC-IN-3 is a dual inhibitor targeting histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs). It exhibits potent and selective activity, with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28 nM, and 82.87 nM against CDK9, CDK12, CDK13, HDAC1, HDAC2, and HDAC3, respectively. This compound is particularly relevant for research in acute myeloid leukemia (AML), providing insights into therapeutic strategies for this disease.

Cat. No.

A26454

CAS No.

1834513-65-3

Bocodepsin

Synonyms: OKI-179

Bocodepsin is a selective inhibitor of histone deacetylases (HDACs) that exhibits significant antitumor activity. This orally active compound is effective against both solid tumors and hematologic malignancies, making it a valuable tool in cancer research. Bocodepsin's mechanism of action involves the modulation of gene expression and apoptosis, contributing to its potential therapeutic applications in oncology.

Cat. No.

A26456

CAS No.

2121516-17-2

HDAC1/2-IN-3

HDAC1/2-IN-3 is a potent inhibitor of histone deacetylases 1 and 2 (HDAC1 and HDAC2), demonstrating IC50 values of 0-5 nM and 5-10 nM, respectively. This compound plays a significant role in modulating gene expression by disrupting histone deacetylation, making it useful in research applications related to cancer biology, neurodegenerative disorders, and epigenetic modifications. Its high selectivity and potency make it a valuable tool for investigating the mechanisms of HDAC-related pathways.

Cat. No.

A26471

CAS No.

2831230-38-5

SHP2/HDAC-IN-1

SHP2/HDAC-IN-1 is a dual allosteric inhibitor targeting SHP2 and HDAC with IC50 values of 20.4 nM and 25.3 nM, respectively. This compound enhances antitumor immunity through the activation of T cells, improving antigen presentation and cytokine secretion. SHP2/HDAC-IN-1 is valuable for investigations in cancer immunotherapy and associated research applications.

Cat. No.

A26475

CAS No.

1267502-34-0

FNDR-20123 free base

FNDR-20123 free base is a potent, orally active anti-malarial agent that functions as a histone deacetylase (HDAC) inhibitor. It demonstrates significant inhibitory activity against Plasmodium falciparum, achieving IC50 values of 41 nM during the asexual stage and 190 nM for male gametocytes. In addition, FNDR-20123 free base selectively inhibits various HDAC isoforms, including HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, with respective IC50 values of 25 nM, 29 nM, 2 nM, 11 nM, and 282 nM. This compound is a valuable tool for research into the treatment of malaria and the role of HDACs in cellular regulation.

Cat. No.

A26477

CAS No.

1315334-23-6

OKI-006

OKI-006 is a potent, orally active inhibitor of histone deacetylase (HDAC). As a unique congener of the natural product HDAC inhibitor largazole, it modulates epigenomic regulation by targeting HDACs, enzymes integral to histone acetylation, which is often dysregulated in various cancers. This compound demonstrates significant potential for research applications in cancer biology and the study of epigenetic alterations in tumorigenesis.

Cat. No.

A26480

CAS No.

1834513-66-4

Bocodepsin hydrochloride

Synonyms: OKI-179 hydrochloride

Bocodepsin hydrochloride is a selective histone deacetylase (HDAC) inhibitor that demonstrates notable antitumor activity. It is effective in the suppression of solid tumors as well as hematologic malignancies, making it a valuable tool for cancer research. Bocodepsin hydrochloride is suitable for studies aimed at elucidating the role of HDAC in tumor biology and therapeutic response.

Cat. No.

A26482

CAS No.

2669785-84-4

JPS035

JPS035 is a benzamide-derived HDAC degrader that utilizes the Von Hippel-Lindau (VHL) E3 ligase-mediated PROTAC technology. It specifically targets and degrades class I histone deacetylases (HDAC1 and HDAC2), leading to significant alterations in gene expression and promoting apoptosis in HCT116 colorectal cancer cells. This compound serves as a valuable tool for studies focused on epigenetic modulation and therapeutic strategies against HDAC-related diseases.

Cat. No.

A26484

CAS No.

763066-77-9

HDAC-IN-72

HDAC-IN-72 is a potent inhibitor of histone deacetylases 1 (HDAC1), 2 (HDAC2), and 3 (IC50 values of 0.65 μM, 0.78 μM, and 1.70 μM, respectively). This compound exhibits significant antiproliferative activity, making it a valuable tool for studying epigenetic regulation in cancer. HDAC-IN-72 is particularly relevant for breast cancer research, facilitating investigations into the role of histone deacetylation in tumor biology and potential therapeutic strategies.

Cat. No.

A26485

CAS No.

2484255-65-2

HDAC6/8/BRPF1-IN-1

HDAC6/8/BRPF1-IN-1 is a selective dual inhibitor targeting HDAC6, HDAC8, and the bromodomain and PHD finger-containing protein 1 (BRPF1). It demonstrates inhibitory activity against HDAC1, HDAC6, and HDAC8 with IC50 values of 797 nM, 344 nM, and 908 nM, respectively, while also inhibiting BRPF1 with a Kd value of 175.2 nM. This compound is valuable for research in cancer biology, providing insights into the role of histone deacetylases and bromodomain proteins in tumorigenesis and cellular processes.

Cat. No.

A26487

CAS No.

2669785-77-5

JPS016

JPS016 is a class I histone deacetylase (HDAC) PROTAC inhibitor that targets HDAC1, HDAC2, and HDAC3 for ubiquitination and proteasomal degradation via VHL E3 ligase recruitment. This compound demonstrates significant anticancer activity by reducing the viability of colon cancer cells and inducing apoptosis. Additionally, JPS016 activates the PINK1/Parkin-mediated mitochondrial autophagy pathway, enhancing cardiomyocyte viability, alleviating mitochondrial damage, and decreasing mitochondrial ROS production. It is valuable for research into colon cancer and sepsis-related cardiac dysfunction.

Cat. No.

A26488

CAS No.

2798954-66-0

STR-V-53

STR-V-53 is a histone deacetylase (HDAC) inhibitor with a low nanomolar IC50. By inhibiting HDAC activity, STR-V-53 increases histone acetylation, leading to altered gene expression. This compound exhibits significant anti-tumor properties, inhibiting proliferation and promoting apoptosis in cancer cells. It serves as a valuable research tool for studying epigenetic regulation and potential therapeutic strategies in oncology.