HDAC1

Cat. No.

A31947

CAS No.

2928537-98-6

DLC-50

DLC-50 is a dual inhibitor of PARP-1 and HDAC-1, exhibiting IC50 values of 1.2 nM and 31 nM, respectively. This compound effectively inhibits the proliferation of various breast cancer cell lines, including MDA-MB-436, MDA-MB-231, and MCF-7, with IC50 values of 0.3, 2.7, and 2.41 μM. Additionally, DLC-50 induces apoptosis specifically in MDA-MB-231 cells and causes cell cycle arrest at the G2 phase, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A31948

CAS No.

2197029-81-3

CDK9/HDAC1/HDAC3-IN-1

CDK9/HDAC1/HDAC3-IN-1 is a dual inhibitor targeting CDK9 and HDACs. With IC50 values of 0.17 μM for CDK9, 1.73 μM for HDAC1, and 1.11 μM for HDAC3, this compound effectively disrupts the activity of these proteins. It induces cancer cell apoptosis and causes cell cycle arrest at the G2/M phase. Additionally, CDK9/HDAC1/HDAC3-IN-1 exhibits broad-spectrum anti-cancer effects, demonstrating efficacy against various malignancies, including breast, cervical, and liver cancers, as evidenced in murine TNBC MDA-MB-231 xenograft models.

Cat. No.

A31953

CAS No.

3069195-42-9

ZWZH-21

ZWZH-21 is a selective inhibitor of histone deacetylases HDAC1 and HDAC2, demonstrating IC50 values of 34 nM and 41 nM, respectively. This dual-action compound exhibits potent anti-proliferative effects on colorectal cancer cell lines HCT116 and SW480, with IC50 values of 0.524 μM and 1.063 μM, respectively. Additionally, ZWZH-21 effectively inhibits cell migration and prompts apoptosis in multiple colorectal cancer models, making it a valuable tool for cancer research, particularly in the study of colorectal cancer.

Cat. No.

A31998

CAS No.

1013620-98-8

ST13

ST13 is a selective inhibitor of HDAC1 and HDAC2, exhibiting IC50 values of 23 nM and 49 nM, respectively. It offers weak inhibition of HDAC3 and HDAC6, with IC50 values of 4.30 μM and >10 μM, respectively. The binding mechanism of ST13 involves an initial rapid formation of a collision complex followed by a slow conversion to a stable complex. This compound has demonstrated the ability to induce apoptosis in cancer cells and is useful for research on melanoma and triple-negative breast cancer.

Cat. No.

A32026

CAS No.

2414921-48-3

PDE5/HDAC-IN-1

PDE5/HDAC-IN-1 is a dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDAC) with IC50 values of 46.3 nM and 14.5 nM, respectively. This compound has demonstrated the capability to induce cell apoptosis and exhibits significant anticancer activities. PDE5/HDAC-IN-1 is a valuable tool for research in cancer therapeutics and epigenetic modulation.

Cat. No.

A32036

CAS No.

2559747-12-3

JPS004

JPS004 is a targeted proteolysis targeting chimera (PROTAC) that degrades histone deacetylases HDAC1-3. By inducing the degradation of these enzymes, JPS004 facilitates histone acetylation, which can promote apoptosis in cancer cells. This compound is valuable for research into cancer biology and therapeutic strategies aimed at modulating epigenetic modifications.

Cat. No.

A32065

CAS No.

2284460-01-9

MC2590

MC2590 is a selective histone deacetylase (HDAC) inhibitor that targets class I and IIb HDAC isoforms, including HDAC1-3, -6, -8, and -10, with IC50 values ranging from 0.015 μM to 0.156 μM. It also inhibits other HDAC isoforms, such as HDAC4, HDAC5, HDAC7, HDAC9, and HDAC11, with higher IC50 values between 1.35 μM and 3.98 μM. MC2590 has been shown to induce G2/M cell cycle arrest and influences the expression of pro- and anti-apoptotic microRNAs, leading to the induction of apoptosis. This compound is valuable for research in cancer biology, epigenetics, and cell cycle regulation.

Cat. No.

A32097

CAS No.

2580938-58-3

CDK/HDAC-IN-2

CDK/HDAC-IN-2 is a dual inhibitor of histone deacetylases (HDACs) and cyclin-dependent kinases (CDKs), exhibiting IC50 values of 6.4 nM for HDAC1, 0.25 nM for HDAC2, 45 nM for HDAC3, and >1000 nM for HDAC6,8, as well as 8.63 nM for CDK1, 0.30 nM for CDK2, and >1000 nM for CDK4,6,7. This compound demonstrates significant antiproliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. CDK/HDAC-IN-2 is particularly valuable in cancer research due to its potent antitumor efficacy.

Cat. No.

A32120

CAS No.

2995354-52-2

HDAC-IN-71

HDAC-IN-71 is a potent histone deacetylase (HDAC) inhibitor that exhibits IC50 values of 12.6 nM for HDAC1, 14.1 nM for HDAC2, 20 nM for HDAC3, 3 nM for HDAC6, and 72 nM for HDAC10. This compound effectively induces apoptosis, making it a valuable tool in cancer research. Its selective inhibition of multiple HDAC isoforms can aid in elucidating the role of histone modification in tumor progression and therapeutic response.

Cat. No.

A32131

CAS No.

2966782-82-9

LSD1/HDAC-IN-2

LSD1/HDAC-IN-2 is a potent inhibitor of lysine-specific demethylase 1 (LSD1) and several histone deacetylases (HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8), with IC50 values ranging from 1.0 to 39.0 nM. This compound demonstrates significant biological activity by inhibiting the proliferation of colorectal cancer cells, inducing apoptosis, and causing G2/M cell cycle arrest. Additionally, LSD1/HDAC-IN-2 reduces cell migration and displays antitumor efficacy in mouse models, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A32153

CAS No.

2454024-18-9

HDAC-IN-42

HDAC-IN-42 is a potent and selective inhibitor of histone deacetylases (HDACs), displaying IC50 values of 0.19 µM for HDAC1 and 4.98 µM for HDAC6. This compound demonstrates significant anticancer and anti-proliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. HDAC-IN-42 is valuable for research applications focused on cancer biology and the modulation of gene expression through epigenetic mechanisms.

Cat. No.

A32165

CAS No.

2920046-95-1

HDAC-IN-63

HDAC-IN-63 is a dual inhibitor targeting both FLT3 and HDAC, with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It demonstrates potent inhibition of MV4-11 cell proliferation, with an IC50 of 92 nM, and effectively induces apoptosis while arresting the cell cycle in MV4-11 cells. This compound serves as a valuable research tool for the study of acute myeloid leukemia (AML) and the exploration of novel therapeutic strategies.

Cat. No.

A32240

CAS No.

2864394-30-7

FLT3/HDAC-IN-3

FLT3/HDAC-IN-3 is a dual inhibitor targeting FLT3 and HDAC, with a potent inhibitory effect on FLT3 (IC50 = 14 nM) and HDAC isoforms, including HDAC1 (IC50 = 27 nM) and HDAC6 (IC50 = 20 nM). This compound demonstrates selective inhibition, exhibiting reduced activity against HDAC8 and no activity toward HDAC4. FLT3/HDAC-IN-3 has shown anti-proliferative effects across various hematological malignancy cell lines and demonstrates efficacy in the Jeko-1 xenograft model without significant toxicity. It is suitable for research focused on hematological malignancies and the role of dual inhibition in therapeutic strategies.

Cat. No.

A32256

CAS No.

2787560-44-3

HDAC-IN-81

HDAC-IN-81 is a potent HDAC1 inhibitor, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-cancer activity by effectively inhibiting cell proliferation and inducing apoptosis in cancer cells. It serves as a valuable tool for research applications in cancer biology and epigenetic regulation.

Cat. No.

A32257

CAS No.

62959-43-7

Valproic acid magnesium

Synonyms: Magnesium valproate; VPA magnesium; 2-Propylpentanoic acid magnesium

Valproic acid magnesium is an orally active histone deacetylase (HDAC) inhibitor that exhibits an IC50 range of 0.5 to 2 mM, specifically inhibiting HDAC1 with an IC50 of 400 μM while promoting the proteasomal degradation of HDAC2. This compound activates Notch1 signaling and demonstrates anti-proliferative effects in small cell lung cancer (SCLC) cells. Valproic acid magnesium has diverse therapeutic applications, including the treatment of epilepsy, bipolar disorder, metabolic diseases, HIV infection, and the prevention of migraine headaches.

Cat. No.

A32276

CAS No.

1256448-48-2

Nanatinostat TFA

Synonyms: CHR-3996 TFA

Nanatinostat TFA is a potent, orally active inhibitor of class I histone deacetylases (HDACs), with IC50 values of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. It demonstrates reduced activity against HDAC5 and HDAC6, with IC50 values of 200 nM and 2100 nM, respectively. Nanatinostat TFA effectively induces apoptosis in myeloma cells and exhibits significant anticancer properties against various malignancies, including advanced solid tumors and colorectal cancer. Its selective inhibition of HDACs positions it as a valuable compound for cancer research and therapeutic development.

Cat. No.

A32281

CAS No.

1401998-36-4

Fimepinostat mesylate

Synonyms: CUDC-907 mesylate

Fimepinostat mesylate is a potent dual inhibitor targeting class I phosphoinositide 3-kinases (PI3Ks) and histone deacetylases (HDACs). It exhibits IC50 values of 19 nM for PI3Kα, 54 nM for PI3Kβ, 39 nM for PI3Kδ, and 1.7 nM for HDAC1, 5.0 nM for HDAC2, 1.8 nM for HDAC3, and 2.8 nM for HDAC10. This compound is valuable for research applications focusing on cancer biology, epigenetic regulation, and cellular signaling pathways.

Cat. No.

A32323

CAS No.

1620054-84-3

WJ35435

WJ35435 is a dual-target HDAC and topoisomerase I inhibitor that exerts anticancer activity by inducing DNA damage and promoting cell cycle arrest at the G1 and G2 phases, ultimately leading to apoptosis. This compound enhances histone H3 acetylation and phosphorylation, along with α-tubulin acetylation and the formation of γ-H2AX, thereby effectively demonstrating its anti-HDAC properties. WJ35435 holds potential for advancing research in cancer therapeutics.

Cat. No.

A32378

CAS No.

2562386-85-8

HDAC-IN-46

HDAC-IN-46 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.21 μM for HDAC1 and 0.021 μM for HDAC6. In MDA-MB-231 cells, HDAC-IN-46 promotes the upregulation of phosphorylated p38 while downregulating Bcl-xL and cyclin D1, leading to significant G2 phase cell cycle arrest and apoptosis. This compound is valuable for research focused on triple-negative breast cancer (TNBC).

Cat. No.

A32436

CAS No.

2716217-79-5

HDAC-IN-57

HDAC-IN-57 is a potent orally active inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 2.07 nM for HDAC1, 4.71 nM for HDAC2, 2.4 nM for HDAC6, and 107 nM for HDAC8. In addition, HDAC-IN-57 inhibits lysine-specific demethylase 1 (LSD1) with an IC50 of 1.34 µM. This compound induces apoptosis and demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development targeting epigenetic regulation.

Cat. No.

A37617

CAS No.

937727-03-2

MRLB-223

MRLB-223 is a selective inhibitor of HDAC1 and HDAC2, demonstrating potent activity against tumor cells. It induces histone hyperacetylation and activates the intrinsic apoptotic pathway, leading to tumor cell apoptosis and degradation of Bcr-Abl in a caspase-dependent manner. Notably, MRLB-223 mediates p53-independent cell death in Bcr-Abl-expressing myeloid cells and shows efficacy in animal models of Eμ-myc lymphoma. This compound is valuable for research focusing on the mechanisms of lymphomagenesis and therapeutic strategies for Eμ-myc lymphoma.

Cat. No.

A43762

CAS No.

1616863-09-2

HDAC-IN-101

HDAC-IN-101 is a selective inhibitor of HDAC1, exhibiting an IC50 of 65 nM against human HDAC1. This compound effectively inhibits cancer cell proliferation by targeting HDAC1 activity. In addition, HDAC-IN-101 is metabolically activated by overexpressed nitroreductase to produce H6AQ, which displays fluorescence under low pH conditions. Its unique properties make it valuable for applications in cancer research and cellular imaging studies.

Cat. No.

A57720

CAS No.

2256079-52-2

CM-444

CM-444 is a potent inhibitor of histone deacetylases (HDACs) with an IC50 range of 6 nM to 0.6 μM, and demonstrates inhibition of DNA methyltransferases (DNMT) with IC50 values between 1.8 and 2.3 μM. This compound facilitates the differentiation of acute myeloid leukemia cells and exhibits significant anti-leukemic activity, enhancing survival rates in mouse models. CM-444 serves as a valuable tool for research into cancer epigenetics and the development of targeted therapies for leukemia.

Cat. No.

A55007

CAS No.

2098896-13-8

HDAC-IN-54

HDAC-IN-54 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 25 nM for human HDAC1, 66 nM for HDAC2, 6.5 nM for HDAC3, and 281 nM for HDAC6. This compound effectively induces acetylation of α-tubulin and histone H3, promoting cancer cell apoptosis, particularly in synergy with cisplatin. HDAC-IN-54 is relevant for research applications in head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma.

Cat. No.

A12758

CAS No.

1316215-12-9

Citarinostat (ACY-241)

Synonyms: HDAC-IN-2; ACY-241

ACY-241 is a new, selective and orally available inhibitor of HDAC6.