HDAC Inhibitor

HDAC/HSP90-IN-1 (compound 20) is a potent dual inhibitor of HDAC (IC₅₀ = 194 nM) and HSP90 (HSP90α IC₅₀ = 153 nM). HDAC/HSP90-IN-1 induces HSP70 expression, downregulates HSP90 client proteins, and promotes acetylation of α-tubulin and histone H3 in cancer cells. HDAC/HSP90-IN-1 reduces PD-L1 expression in IFN-γ treated H1975 cells. HDAC/HSP90-IN-1 can be used for cancer research, such as lung and colon cancer.

Nanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC₅₀s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC₅₀ of 200 nM) and HDAC6 (IC₅₀ of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.

HDAC/HSP90-IN-2 (compound 26) is a potent dual inhibitor of HDAC (IC₅₀ = 360 nM) and HSP90 (HSP90α IC₅₀ = 77 nM). HDAC/HSP90-IN-2 induces HSP70 expression, downregulates HSP90 client proteins, and promotes acetylation of α-tubulin and histone H3 in cancer cells. HDAC/HSP90-IN-2 reduces PD-L1 expression in IFN-γ treated H1975 cells. HDAC/HSP90-IN-2 can be used for cancer research, such as lung and colon cancer.

HDAC-IN-74 (PA) is a dual HDAC/Rribonucleotide reductase(RR) inhibitor, with IC₅₀ values ​​of 10.80 μM and 9.34 μM for HDAC and HDAC, respectively. HDAC-IN-74 can be used in anticancer research.

HDAC/HSP90-IN-3 (compound J5) is a potent and selective fungal Hsp90 and HDAC dual inhibitor, with IC₅₀ values of 0.83 and 0.91 μM, respectively. HDAC/HSP90-IN-3 shows antifungal activity against azole resistant C. albicans. HDAC/HSP90-IN-3 can suppress important virulence factors and down-regulate drug-resistant genes ERG11 and CDR1.

HDAC-IN-104 is a potent and selective class I Histone deacetylases (HDAC) inhibitor with an IC₅₀ of 25 nM. HDAC-IN-104 exerts potent antiproliferative and antitumor effects by inhibiting glycolysis and OXPHOS via blockade of the PI3K/AKT signaling pathway, and these effects are synergistically enhanced when combined with the FMS-like tyrosine kinase 3 (FLT3) inhibitor Quizartinib (AC220) (HY-13001). HDAC-IN-104 induces significant early and late apoptosis. HDAC-IN-104 can be used for acute myeloid leukemia (AML) research.

HDAC-IN-68 (hydrochloride) (Compound 29) has inhibitory activity against HDACs (IC₅₀=0.04 μM) and fragments microtubules by activating katanin, a microtubule-severing protein. HDAC-IN-68 (hydrochloride) can be used in cancer research.

COX-2-IN-23 (compound A10) is a potent both AChE and HDAC inhibitor with IC₅₀ values of 0.12 and 0.23 nM. COX-2-IN-23 exhibits antioxidant activity and metal chelating properties. COX-2-IN-23 can be used in alzheimer's disease research.

JAK/HDAC-IN-2 is a potent 2-amino-4-phenylaminopyrimidine JAK/HDAC dual-target inhibitor. JAK/HDAC-IN-2 potently inhibits HDAC3/6 and JAK1/2 at nanomolar levels. JAK/HDAC-IN-2 has proapoptotic activity and inhibits histone deacetylation and STAT3 phosphorylation. JAK/HDAC-IN-2 presents remarkable antiproliferative activity in both hematological malignancies and solid cancers.

PIM-1/HDAC-IN-1 (compound 4d) is a PIM-1 inhibitor, with an IC₅₀ of 343.87 nM. PIM-1/HDAC-IN-1 has strong inhibitory activity and selectivity against HDAC 1 and HDAC 6, with IC₅₀ values of 63.65 and 62.39 nM, respectively. PIM-1/HDAC-IN-1 exhibits apoptosis inducing potential in MCF-7 cell lines. PIM-1/HDAC-IN-1 shows pre-G1 apoptosis and cell cycle arrest at G2/M phase.

VEGFR2/HDAC1-IN-1 (compound 13) is a potent VEGFR-2/HDAC dual inhibitor, with IC₅₀s of 57.83 nM and 9.82 nM, respectively. VEGFR2/HDAC1-IN-1 arrests the cell cycle at the S and G2 phases, and induces apoptosis in HeLa cells. VEGFR2/HDAC1-IN-1 exhibits anti-angiogenic effect.

YPX-C-05 is an orally active HDAC inhibitor and vasodilator. YPX-C-05 inhibits HDAC enzymatic activity, increases histone H₄ acetylation, activates the PI3K/Akt pathway, promotes Akt and eNOS phosphorylation, enhances eNOS activity, and boosts nitric oxide production. YPX-C-05 increases Tetrahydrobiopterin (HY-107383) levels, restores serum nitric oxide levels, reduces endothelin-1 levels, and improves endothelial function. YPX-C-05 reduces vascular remodeling and exerts antihypertensive effects in hypertensive Mus musculus mice. YPX-C-05 can be used for the research of hypertension.

1-Alaninechlamydocin, a cyclic tetrapeptide, is a potent HDAC inhibitor (IC₅₀=6.4 nM). 1-Alaninechlamydocin induces G2/M cell cycle arrest and apoptosis in MIA PaCa-2 cells.

PB118 is a potent inhibitor of HDAC6 that plays an important role in the pathophysiology of Alzheimer's disease.

HDAC6-IN-56 (compound 18d) is an inhibitor of HDAC6 with an IC₅₀ of 1.3 nM. HDAC6-IN-56 suppresses S phase and induces apoptosis in HCT-116 colon cancer cells.

FLT3/HDAC-IN-1 is a dual inhibitor of FLT3/HDAC, with IC₅₀ values of 30.4, 52.4, and 14.7 nM for FLT3, HDAC1, and HDAC3, respectively. FLT3/HDAC-IN-1 can induce apoptosis in MV-4-11 cells and has anti-proliferative effects on FLT3 mutant-transformed BaF3 cells. FLT3/HDAC-IN-1 is being researched for its potential in treating hard-to-treat solid tumors and hematological malignancies.

HDAC6-IN-24 (compound N1) is a inhibitor of HDAC6.

STR-V-53 is an HDAC inhibitor (IC₅₀ in nM).STR-V-53 increases histone acetylation in tumor cells by inhibiting the activity of these enzymes, which in turn regulates gene expression.STR-V-53 inhibits tumor growth, and induces apoptosis.

HDAC6-IN-32 (compound 25202) is a selective and potent inhibitor of HDAC6. HDAC6-IN-32 blocks HDAC6 activity and interferes with microtubule dynamics, leading to SAC activation and prolonged mitotic arrest, ultimately leading to apoptosis in CRPC cells.

IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.