HDAC Inhibitor

Pomiferin (NSC 5113) acts as an potential inhibitor of HDAC, with an IC₅₀ of 1.05 μM, and also potently inhibits mTOR (IC₅₀, 6.2 µM).

Bakkenolide A is an anticancer agent. Bakkenolide A reduces the viability of leukemia cells, inhibits cell colony formation and invasion, and downregulates the expression of HDAC3 in cells. Bakkenolide A downregulates the expression of pro-inflammatory cytokines including TNF-α, interleukins such as IL-1β, TGF-β1 and IFN-γ, as well as the expression of PI3K, PDK and PKC in leukemia cells. Bakkenolide A downregulates activated Akt, GSK and Bad, while upregulates Cyto-c, cleaved Caspase3 and cleaved Caspase7, induces apoptosis (apoptosis) in leukemia cells and thereby inhibits inflammatory responses in leukemia cells. Bakkenolide A significantly slows the growth of subcutaneous leukemia tumors in nude mice. Bakkenolide A is applicable to leukemia-related research.

HDAC10-IN-2 hydrochloride (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC₅₀ of 20 nM. HDAC10-IN-2 hydrochloride modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells.

HDAC1 Human Pre-designed siRNA Set A contains three designed siRNAs for HDAC1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

Panobinostat (Standard) (LBH589 (Standard)) is the analytical standard of Panobinostat (HY-10224). This product is intended for research and analytical applications. Panobinostat is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma.

Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias.

Valproic acid-d₆ is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an 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 activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

Phenylbutyrate-d₁₁ (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.

RSC133 is a dual inhibitor of DNA methyltransferase 1 and histone deacetylase 1 inhibitor. RSC133 promotes cell proliferation, up-regulates H₃K₉ histone acetylation, down-regulates p53, p21, p16/INK4A, and ablates pro-senescence phenotypes.

Bocodepsin (OKI-179) is an orally active and selective HDAC inhibitor, with antitumor activity. Bocodepsin can be used for suppression on solid tumor and hematologic malignancies.

Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC₅₀s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.

Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research.

Martinostat hydrochloride is a HDAC inhibitor and can be labeled with radionuclides for quantitative imaging of HDACs in vivo in the central nervous system and major peripheral organs.

MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI₅₀ of 0.03 μM.

4-Phenylbutyric acid-d₁₁ is the deuterium labeled 4-Phenylbutyric acid. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.

KD 5170 is a pan inhibitor of histone deacetylases (HDACs) and exhibits broad spectrum antitumor activity in vitro and in vivo.

HDAC11 Human Pre-designed siRNA Set A contains three designed siRNAs for HDAC11 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

F-SAHA is a HDAC inhibitor (HDACi) and its ¹⁸F labeled derivative can be used in tumor imaging research.

Valproic acid-d₄ is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an 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 activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.

JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC₅₀s of 4 and 2 nM for JAK2 and HDAC, respectively.