HDAC Inhibitor

SR-4370 is an inhibitor of HDAC, with IC₅₀s of 0.13 μM, 0.58 μM, 0.006 μM, 2.3 μM, and 3.4 μM for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, respectively.

9-Hydroxyoctadecanoic acid (9-HSA) is an HDAC1 inhibitor that inhibits ∼66.4% HDAC1 enzymatic activity at 5 μM. 9-Hydroxyoctadecanoic acid shows anticancer activity.

DKFZ-748 is a selective HDAC10 inhibitor (pIC₅₀=7.66), and shows anti-tumor activity.

Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC₅₀s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity.

Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2 and histone deacetylase 2 (HDAC2). Rhamnetin exhibits antitumor, antioxidant and anti-inflammatory activity.

Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the research of AML.

Vorinostat (Standard) is the analytical standard of Vorinostat. This product is intended for research and analytical applications. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID₅₀ values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.

TH34, an HDAC6/8/10 inhibitor with IC₅₀s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.

ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC₅₀ of 7.5 nM. ACY775 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).

HDAC8-IN-1 is a HDAC8 inhibitor with an IC₅₀ of 27.2 nM.

HDAC10-IN-1 (compound 13b) is a potent and highly selective HDAC10 inhibitor, with an IC₅₀ of 58 nM. HDAC10-IN-1 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells.

HDAC2-IN-2 (compound 124) is an inhibitor of HDAC2 with Kd value of 0.1-1 μM.

Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC₅₀ of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).

Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC₅₀ values of 6 nM, 9 nM, 9 nM and 25 nM, respectively.

ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC₅₀ of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.

ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC₅₀s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9.

Droxinostat (NS 41080) is a histone deacetylase (HDAC) inhibitor. Droxinostat selectively inhibits HDAC3, HDAC6, and HDAC8 with IC₅₀ values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively. Droxinostat can be used for the research of hepatocellular carcinoma (HCC).

Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC₅₀ of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC₅₀ of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.

BML-210 is a potent HDAC inhibitor. BML-210 can inhibit the HDAC4-VP16-driven reporter signal with an apparent IC₅₀ of ∼5 µM. BML-210 has a specific disruptive effect on the HDAC4:MEF2 interaction. BML-210 causes an increase in the G0/G1 phase. BML-210 induces apoptosis and displays antitumour activities in orthotopic mammary tumours in mice.

T-518 is an orally active, BBB-penetrant and potent DFMO-based HDAC6 inhibitor with high selectivity (IC₅₀ = 36 nM). T-518 improves axonal transport. T-518 ameliorates object recognition deficit. T-518 can be studied in research for Alzheimer’s disease and tauopathy.