HDAC1

Cat. No.

A31695

CAS No.

2727102-12-5

Aurora kinase/HDAC-IN-1

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.

Cat. No.

A31716

CAS No.

2987905-95-1

HDAC1/CDK7-IN-1

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.

Cat. No.

A31720

CAS No.

2416914-29-7

WMJ-J-09

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.

Cat. No.

A31730

CAS No.

3031349-25-1

TH-6

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.

Cat. No.

A31783

CAS No.

68676-88-0

Trichostatin C

Trichostatin C is an HDAC inhibitor that plays a crucial role in modulating gene expression by preventing the deacetylation of histones. This compound exhibits significant anticancer activity, inducing apoptosis and causing cell cycle arrest in the G2/M phase, making it particularly effective against lung cancer and urothelial bladder cancer. Additionally, Trichostatin C promotes differentiation in Friend leukemic cells and demonstrates antifungal properties, highlighting its potential in various research applications related to cancer biology and fungal infections.

Cat. No.

A31809

CAS No.

2883046-06-6

JMJD3/HDAC-IN-1

JMJD3/HDAC-IN-1 is a dual inhibitor targeting both Jumonji domain-containing protein demethylase 3 (JMJD3) and histone deacetylases HDAC1 and HDAC6. With an IC50 value of 16 nM for HDAC1, this compound induces hypermethylation of histone H3K27 and hyperacetylation of H3K9, promoting apoptosis through cleavage of caspase-7 and PARP. JMJD3/HDAC-IN-1 demonstrates significant anti-cancer activity by inhibiting cell cloning, migration, and invasion, making it valuable in cancer research and therapeutic studies.

Cat. No.

A30663

CAS No.

960055-56-5

Panobinostat lactate

Synonyms: LBH589 lactate; NVP-LBH589 lactate

Panobinostat lactate is a potent, orally active non-selective histone deacetylase (HDAC) inhibitor. It exhibits significant antineoplastic activity and has been shown to disrupt HIV latency effectively. Additionally, Panobinostat lactate induces apoptosis and autophagy in various cell types. This reagent is valuable for studying refractory or relapsed multiple myeloma and exploring HDAC inhibition in cancer research.

Cat. No.

A30803

CAS No.

2650188-32-0

Purinostat mesylate

Purinostat mesylate is a selective inhibitor of histone deacetylases (HDACs), effectively targeting class I and class IIb HDACs with IC50 values ranging from 0.81 to 11.5 nM. This compound induces apoptosis and influences the cell cycle in LAMA84 and 188 BL-2 cell lines, demonstrating potent anti-leukemic effects in vivo. Purinostat mesylate serves as a valuable tool for researching lymphoblastic leukemia and its therapeutic potential.

Cat. No.

A32517

CAS No.

2766466-56-0

HDAC-IN-37

HDAC-IN-37 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.0551 μM for HDAC1, 1.24 μM for HDAC3, 0.948 μM for HDAC8, and 34.2 μM for HDAC6. This compound effectively increases histone acetylation through a slow-off binding mechanism. Additionally, HDAC-IN-37 disrupts the transition from the G1 phase to the S phase of the cell cycle and promotes early apoptosis in various cell types, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A32525

CAS No.

2439175-23-0

c-Met/HDAC-IN-3

c-Met/HDAC-IN-3 is a dual inhibitor targeting c-Met and histone deacetylase 1 (HDAC1), exhibiting IC50 values of 12.50 nM and 26.97 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. c-Met/HDAC-IN-3 serves as a valuable tool for research in cancer biology and therapeutic development, particularly in studies focused on synergistic inhibition of oncogenic pathways.

Cat. No.

A32535

CAS No.

1916505-13-9

HDAC-IN-31

HDAC-IN-31 is a selective and orally active histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 84.90 nM for HDAC1, 168.0 nM for HDAC2, 442.7 nM for HDAC3, and greater than 10,000 nM for HDAC8. This compound induces apoptosis and triggers G2/M phase cell cycle arrest, demonstrating significant antitumor efficacy. HDAC-IN-31 is applicable in research focused on diffuse large B-cell lymphoma and other cancer studies.

Cat. No.

A32554

CAS No.

2775446-49-4

Top/HDAC-IN-1

Top/HDAC-IN-1 is a dual inhibitor targeting both topoisomerase and histone deacetylases (HDACs), demonstrating IC50 values of 18 nM for HDAC1, 230 nM for HDAC2, 790 nM for HDAC3, 87 nM for HDAC6, and 5250 nM for HDAC8. This compound exhibits significant antitumor activity against HCT116 cells, with an IC50 of 180 nM, effectively inducing apoptosis and promoting G2 cell cycle arrest. Top/HDAC-IN-1 serves as a valuable tool in cancer research, particularly for studies involving epigenetic modulation and cell proliferation.

Cat. No.

A32625

CAS No.

2740495-53-6

c-Met/HDAC-IN-2

c-Met/HDAC-IN-2 is a highly potent dual inhibitor targeting c-Met and histone deacetylases (HDACs), exhibiting IC50 values of 18.49 nM for HDAC1 and 5.40 nM for c-Met. This compound demonstrates significant antiproliferative effects against various cancer cell lines, notably inducing G2/M-phase cell cycle arrest and apoptosis in HCT-116 cells. c-Met/HDAC-IN-2 is a valuable tool for investigating mechanisms of anti-cancer resistance and exploring therapeutic strategies in oncology research.

Cat. No.

A32635

CAS No.

2821923-75-3

HDAC-IN-67

HDAC-IN-67 is a potent inhibitor of histone deacetylases HDAC1 and HDAC6, demonstrating IC50 values of 22 nM and 8 nM, respectively. This compound effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. Its significant antitumor activity makes HDAC-IN-67 a valuable tool for cancer research and a potential candidate for therapeutic development.

Cat. No.

A32639

CAS No.

2897622-19-2

PIM-1/HDAC-IN-1

PIM-1/HDAC-IN-1 is a selective inhibitor of PIM-1 as well as histone deacetylases HDAC 1 and HDAC 6, exhibiting an IC50 of 343.87 nM for PIM-1 and 63.65 nM and 62.39 nM for HDAC 1 and HDAC 6, respectively. This compound demonstrates significant apoptotic activity in MCF-7 cell lines, inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase. PIM-1/HDAC-IN-1 is a valuable tool for research on cancer biology and the regulation of cell proliferation and apoptosis.

Cat. No.

A32642

CAS No.

2653339-26-3

HDAC-IN-50

HDAC-IN-50 is a potent dual inhibitor targeting FGFR and HDAC with IC50 values of 0.18 nM for FGFR1, 1.2 nM for FGFR2, 0.46 nM for FGFR3, 1.4 nM for FGFR4, and varying inhibitory effects on HDAC isoforms such as HDAC1 (1.3 nM), HDAC2 (1.6 nM), HDAC6 (2.6 nM), and HDAC8 (13 nM). This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase. Additionally, HDAC-IN-50 decreases the expression of phosphorylated forms of FGFR1, ERK, and STAT3, indicating its potential applications in cancer research and therapy.

Cat. No.

A32698

CAS No.

3024922-89-9

VEGFR2/HDAC1-IN-1

VEGFR2/HDAC1-IN-1 is a potent dual inhibitor of VEGFR-2 and HDAC, demonstrating IC50 values of 57.83 nM and 9.82 nM, respectively. This compound effectively arrests the cell cycle at the S and G2 phases, leading to apoptosis in HeLa cells. Additionally, VEGFR2/HDAC1-IN-1 exhibits significant anti-angiogenic properties, making it a valuable tool for research in cancer biology and targeted therapies.

Cat. No.

A32715

CAS No.

2857097-33-5

HDAC-IN-34

HDAC-IN-34 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.022 μM for HDAC1 and 0.45 μM for HDAC6. This compound binds to DNA, leading to DNA damage and inducing apoptosis through the p53 signaling pathway. Additionally, HDAC-IN-34 exhibits significant anti-proliferative effects against HCT-116 colorectal cancer cells, with an IC50 of 1.41 μM, making it a valuable tool for cancer research and epigenetic studies.

Cat. No.

A32821

CAS No.

3062141-62-9

HDAC/PSMD14-IN-1

HDAC/PSMD14-IN-1 is a dual-target inhibitor of HDAC1 and PSMD14, exhibiting IC50 values of 238.7 nM and 141.2 nM, respectively. This compound demonstrates significant cytotoxicity against esophageal squamous cell carcinoma (ESCC) cell lines, with IC50 values ranging from 30 to 250 nM. In addition to its ability to induce apoptosis, HDAC/PSMD14-IN-1 effectively reverses epithelial-mesenchymal transition (EMT) and shows promising anti-tumor activity in KYSE30 mouse xenograft models. It is a valuable tool for advancing research in esophageal cancer.

Cat. No.

A32841

CAS No.

141446-96-0

1-Alaninechlamydocin

1-Alaninechlamydocin is a cyclic tetrapeptide that functions as a potent histone deacetylase (HDAC) inhibitor with an IC50 of 6.4 nM. This compound effectively induces G2/M cell cycle arrest and promotes apoptosis in MIA PaCa-2 cells, making it a valuable tool for cancer research. Its activity in modulating epigenetic regulation highlights its potential applications in therapeutic development and studies of cellular differentiation and survival.

Cat. No.

A32846

CAS No.

2763368-89-2

HDAC-IN-27

HDAC-IN-27 is a selective inhibitor of Class I histone deacetylases (HDAC1-3) with an IC50 range of 0.43 to 3.01 nM. It demonstrates significant anti-proliferative and pro-apoptotic effects against acute myeloid leukemia (AML) cell lines by promoting histone acetylation, specifically AcHH3 and AcHH4. This compound is valuable for research into the mechanisms of AML and potential therapeutic applications in histone modification regulation.

Cat. No.

A32868

CAS No.

2630989-02-3

HDAC1/6-IN-1

HDAC1/6-IN-1 is a potent inhibitor targeting HDAC1 and HDAC6, exhibiting IC50 values of 1.3 nM and 13 nM, respectively. This compound effectively inhibits the methylation and deacetylation of H3K9, leading to significant biological activity, including the induction of apoptosis in cancer cells, G0/G1 cell cycle arrest, and the inhibition of cell migration and invasion. It serves as a valuable tool in cancer research and the study of epigenetic regulation.

Cat. No.

A30063

CAS No.

2414046-33-4

HDAC-IN-39

HDAC-IN-39 is a potent inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 1.07 μM for HDAC1, 1.47 μM for HDAC2, and 2.27 μM for HDAC3. This compound also significantly disrupts microtubule polymerization and induces cell cycle arrest at the G2/M phase, highlighting its potential for modulating cell cycle dynamics. Furthermore, HDAC-IN-39 demonstrates promising anticancer activity, particularly against resistant cancer cell lines, making it a valuable tool for cancer research and therapeutic exploration.

Cat. No.

A31905

CAS No.

617690-98-9

SK-7041

SK-7041 is a histone deacetylase (HDAC) inhibitor with an IC50 value of 172 nM. This compound promotes hyperacetylation of histones H3 and H4, leading to the inhibition of tumor cell growth both in vitro and in vivo. Additionally, SK-7041 induces apoptosis and causes cell cycle arrest at the G1 phase, making it a valuable tool for cancer research and therapeutic exploration.

Cat. No.

A31939

CAS No.

3037071-29-4

Wee1/HDAC-IN-1

Wee1/HDAC-IN-1 is a dual inhibitor targeting Wee1 and histone deacetylases (HDACs). It demonstrates potent activity with an IC50 of 1.2 nM for Wee1 and varying IC50 values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. This compound displays significant antiproliferative effects in MV4-11 cells, with an IC50 of 0.076 μM, by disrupting DNA damage repair mechanisms and promoting apoptosis. Wee1/HDAC-IN-1 is suited for research on acute myeloid leukemia (AML).