HDAC Inhibitor

Diheteropeptin has similar activity to T ransforming growth factor-β, and inhibits the ability of HDAC.

Corin (Standard) is the analytical standard of Corin (HY-111048). This product is intended for research and analytical applications. Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a K_i(inact) of 110 nM for LSD1 and an IC₅₀ of 147 nM for HDAC1.

Tubastatin A (Standard) is the analytical standard of Tubastatin A. This product is intended for research and analytical applications. Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).

JNJ-16241199 (Standard) is the analytical standard of JNJ-16241199 (HY-10226). This product is intended for research and analytical applications. JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC₅₀of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21waf1, cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.

(S)-HDAC-IN-102 is a HDAC8 inhibitor and an isomer of HDAC-IN-102 (HY-185554). HDAC-IN-102 inhibits total HDAC with an IC₅₀ of 58 μM and exhibits partial subtype selectivity. Specifically, (S)-HDAC-IN-102 targets HDAC8, while (R)-HDAC-IN-102 (HY-185554B) targets HDAC2. HDAC-IN-102 exerts antioxidant effects by scavenging DPPH free radicals and can be used in cancer-related research.

CUDC-101 (Standard) is the analytical standard of CUDC-101 (HY-10223). This product is intended for research and analytical applications. CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC₅₀s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HDAC6-IN-39 (Compound I-132) is an inhibitor for HDAC6 with IC₅₀ of 0.0096 μM.

β-Hydroxymethyl chalcone is a time-dependent selective HDAC2 inhibitor, with IC₅₀ values of 0.17 μM (24 h) and 9.19 μM (1 h). After binding to the catalytic zinc ion in the active pocket of HDAC2, β-Hydroxymethyl chalcone undergoes an intramolecular nucleophilic attack to form a cyclic product, resulting in time-dependent tight binding. β-Hydroxymethyl chalcone can be used for the study of HDAC2 selective inhibition and related epigenetic targets^[1].

Martinostat 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.

Pracinostat (Standard) is the analytical standard of Pracinostat. This product is intended for research and analytical applications. Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM.

Abexinostat (Standard) is the analytical standard of Abexinostat (HY-10990). This product is intended for research and analytical applications. Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with K_i of 7 nM. Abexinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC₅₀ below 10 nM.

HDAC-IN-2 (Compound 6) is an inhibitor of histone deacetylase 4 (HDAC4). HDAC-IN-2 has affinity for Class IIa enzymes. HDAC-IN-2 is a useful research tool for high-throughput screening and follow-up chemistry.

MMH409 is a selective HDAC8 inhibitor, with an IC₅₀ value of 23 nM and a K_d value of 3.5 nM against human HDAC8, and an IC₅₀ value of 11.64 μM against Schistosoma mansoni HDAC8. MMH409 reduces the viability of newly transformed schistosomula and adult worms of Schistosoma mansoni in vitro. MMH409 serves as a biological probe to investigate the pharmacological knockdown effect of HDAC8 in diseased cells. MMH409 can be used in studies related to neuroblastoma and schistosomiasis.

4-Phenylbutyric acid (Standard) is the analytical standard of 4-Phenylbutyric acid (HY-A0281). This product is intended for research and analytical applications. 4-Phenylbutyric acid (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.

YF438 is an HDAC inhibitor with effective anticancer activity both in vitro and in vivo. YF438 inhibits the growth and metastasis of triple-negative breast cancer (TNBC) cells by blocking the interaction between HDAC and MDM2, inducing the dissociation of MDM2-MDMX, and promoting the degradation of MDM2.

HDAC6-IN-78 (Example 48) is a selective HDAC6 inhibitor with an IC₅₀ of 24 nM. HDAC6-IN-78 shows no activity against other HDAC isoforms.

KBH-A42 is a novel histone deacetylase (HDAC) inhibitor with significant anti-inflammatory properties. KBH-A42 against TNF-α and NO production with IC₅₀ values of 1.10 and 2.71 µM, respectively, in the LPS-induced murine macrophage RAW 264.7 cells.

Tucidinostat (Standard) is the analytical standard of Tucidinostat. This product is intended for research and analytical applications. Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.

Romidepsin-d₇ (FK 228-d₇) is deuterium labeled Romidepsin. Romidepsin (FK 228) is a Histone deacetylase (HDAC) inhibitor with anti-tumor activities. Romidepsin (FK 228) inhibits HDAC1, HDAC2, HDAC4, and HDAC6 with IC₅₀s of 36 nM, 47 nM, 510 nM and 1.4 μM, respectively. Romidepsin (FK 228) is produced by Chromobacterium violaceum, induces cell G2/M phase arrest and apoptosis.

HDAC8-IN-1 (Standard) is the analytical standard of HDAC8-IN-1 (HY-111342). This product is intended for research and analytical applications. HDAC8-IN-1 is a HDAC8 inhibitor with an IC₅₀ of 27.2 nM.