hdaci

BRD-6929 is a selective, brain-penetrant HDAC1 and HDAC2 inhibitor (IC50:  1 and 8 nM). BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 (Kis: 0.2 and 1.5 nM) [2]. BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV

Dioctanoylphosphatidic acid sodium serves as a modulator of phagocyte respiratory bursts, a precursor to diacylglycerol and lyso-phosphatidic acid, and influences the phosphorylation of the mammalian target of rapamycin (mTOR). Additionally, it enhances the viability of gallbladder cancer cells inhibited by histone deacetylase inhibitors (HDACI). This compound is derived from glycerophospholipids through the action of phospholipase D.

Purinostat is a selective inhibitor of HDACI IIb with potential anti-leukemic properties. Its mesylate form, Purinostat mesylate, is effective at inhibiting the survival of Ph+ leukemic cells and CD34+ leukemic cells derived from CML patients. Purinostat mesylate targets HDACI IIb, impacting several crucial factors for leukemia stem cell (LSC) survival, such as c-Myc, β-Catenin, E2f, Ezh2, Alox5, and mTOR. Additionally, Purinostat mesylate enhances glutamate metabolism in LSCs by increasing GLS1.

HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active, HDACI class-selective inhibitor, with IC50 values ranging from 0.43 to 3.01 nM for HDAC1-3. This compound exhibits both in vivo and in vitro anticancer activity. HDAC-IN-27 shows significant antiproliferative effects against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). It is useful for research on acute myeloid leukemia (AML).

ZYJ-25e is an oral histone deacetylase inhibitor (HDACi) with potent antitumor activities.

ZYJ-34c is a potent oral antitumor activities histone deacetylase inhibitor (HDACi).

ZYJ-34v is an oral histone deacetylase inhibitor (HDACi) with potent antitumor activities.

CXD101 is a novel class I-selective HDACi (HDAC1 (IC50 : 63nM), HDAC2 (IC50 :570nM), HDAC3 (IC50 :550nM)). CXD101(CXD-101) has no activity against HDAC class II

HDAC-IN-27 is a potent and orally active inhibitor of HDAC Class I (0.43 nM - 3.01 nM for HDAC1-3). HDAC-IN-27 shows activity against anti-acute myeloid leukemia (AML).

XP5 is a potent, orally active HDAC6 inhibitor (IC50= 31 nM) that inhibits the proliferation of various cancer cell lines, including HDACi-resistant YCC3 7 gastric cancer cells (IC50=0.16-2.31 μM).

Tinostamustine, also known as EDO-S101, is an alkylatlng histone-deacetylase inhibitor (HDACi) fusion molecule. EDO-S101 is a functional pan-histone-deacetylase inhibitor and is assumed to potentiate the alkylating activity of the compound and or may help to overcome resistance to other therapeutic agents.

FFK29 is a synthetic class II HDACi (Histone deacetylase inhibitors) which have have recently emerged as novel therapeutic options for treating various protozoan and parasitic diseases. While these HDACi demonstrated a negligible effect on the viability of mature cysts, Acanthamoeba encystation was significantly inhibited by these HDACi. In conclusion, these synthetic HDACi demonstrated potent amoebicidal effects and inhibited the growth and encystation of Acanthamoeba, thus highlighting their enormous potential for further development.

HDAC4-IN-1 (compound 1a), a class IIa HDACI inhibitor with an IC 50 of 0.077 μM, exhibits anticancer activity by enhancing Caspase-induced apoptosis. It is also utilized in cancer drug combination research [1].

F-SAHA, an HDAC inhibitor (HDACi), and its derivative labeled with 18F are utilized in tumor imaging studies.