HDAC Inhibitor

PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC₅₀ of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT(Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC₅₀=0.17 μM) and has good anti-cancer activity.

LB-205 is a pan-histone deacetylase inhibitor (HDACi). LB-205 can be used for the research of acute traumatic brain injury.

HDAC-IN-58 is a HDAC inhibitor. HDAC-IN-58 has HDAC6-specific inhibition activity with an IC₅₀ value of 2.06 nM. HDAC-IN-58 can be used for the research of chronic diseases, including neurodegenerative and psychiatric conditions.

Panobinostat-d₄ is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].

HDAC8-IN-7 (H7E), a HDAC8 inhibitor, exerts retinoprotective effects against glaucomatous injury via ameliorating aberrant Müller glia activation and oxidative stress. HDAC8-IN-7 alleviates functional and structural defects within the inner retina.

Panobinostat-d₄ (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].

Hdac11 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac11 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), a Valproic acid (HY-10585) derivative, exhibits potential roles of HDAC inhibition (IC₅₀ = 13 μM) and HSP70 induction. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons. 2-Hexyl-4-pentynoic acid can be used for the study of breast carcinoma. 2-Hexyl-4-pentynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Hdac7 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac7 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

GK718 is a HDAC1/3 inhibitor (IC₅₀: 259 and 139 nM respectively). GK718 increased acetylated histone H3 level in cells. GK718 inhibits Bleomycin (HY-108345) induced pulmonary fibrosis in mice.

HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor (IC₅₀: 0.844 and 30.0 nM for FLT3 and HDAC1 respectively). HDAC-IN-63 inhibits MV4-11 cell proliferation (IC₅₀: 92 nM. HDAC-IN-63 induces apoptosis and arrests cell cycle in MV4-11 cells. HDAC-IN-63 can be used for research of acute myeloid leukemia (AML).

HDAC-IN-95 (Compound 9) is a HDAC inhibitor. HDAC-IN-95 can be used for the study of non-small cell lung cancer (NSCLC).

HDAC-IN-66 (compound 2F) is a selective HDAC inhibitor and Pomalidomide (HY-10984) derivative that potently inhibits hematological tumor cells.

AW01178 is a Class I HDAC inhibitor. AW01178 induces the upregulation of E-cadherin at both mRNA and protein levels and inhibits the EMT of breast cancer cells.

Topo II/HDAC-IN-2 (8d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-2 (8d) induces apoptosis.

HDAC-IN-92 is a pan-HDAC inhibitor with an IC₅₀ of 12.58 µM in A2780 cells. HDAC-IN-92 demonstrates broad-spectrum, notable cytotoxic activity against a range of human cancer cell lines, including ovarian, liver, and breast carcinomas. HDAC-IN-92 causes apoptosis and demonstrates a notable decrease in tumor cell colony formation. HDAC-IN-92 inhibits the formation of blood vessels in the chick chorioallantoic membrane (CAM). HDAC-IN-92 exhibits anti-tumor effect in a 4T1 tumor-bearing mouse model. HDAC-IN-92 can be used for research targeting solid tumor.

Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC₅₀ in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC₅₀, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

Mz325 is a dual inhibitor of HDAC and Sirt2, with the IC₅₀ of 9.7 μM to Sirt2, that play an important role in pathogenesis of cancer and neurodegeneration.

Hdac8 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac8 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

Valproic acid magnesium (Magnesium valproate) is an orally active HDAC inhibitor, with IC₅₀ in the range of 0.5 and 2 mM. Valproic acid magnesium inhibits HDAC1 (IC₅₀, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid magnesium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid magnesium is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.