HDAC2 Inhibitor

HDAC-IN-84 (compound 4d) is a potent HDAC inhibitor, with IC₅₀ values of 0.0045, 0.015, 0.013, 0.038, 5.8 and 26 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8 and HDAC11, respectively. HDAC-IN-84 effectively inhibits the proliferation of leukemia cells without causing toxicity.

Quisinostat (JNJ-26481585) hydrochloride is a potent and orally active pan-HDAC inhibitor (HDACi), with IC₅₀ values ranging from 0.11 nM to 0.64 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11. Quisinostat hydrochloride has a broad spectrum antitumoral activity. Quisinostat hydrochloride can induce autophagy in neuroblastoma cells.

HDAC-IN-47 is an orally active inhibitor of histone deacetylase (HDAC), with IC₅₀s of 19.75 nM (HDAC1), 5.63 nM (HDAC2), 40.27 nM (HDAC3), 57.8 nM (HDAC2), 302.73 nM (HDAC8), respectively. HDAC-IN-47 inhibits autophagy and induces apoptosis via the Bax/Bcl-2 and caspase-3 pathways. HDAC-IN-47 arrests cell cycle at G2/M phase, and shows anti-tumor efficacy in vivo.

MRLB-223 is a preferential HDAC1 and HDAC2 inhibitor with activity against tumor cells.MRLB-223 induces histone hyperacetylation, intrinsic apoptotic pathway activation, tumor cell apoptosis, Hsp90 hyperacetylation, and caspase-dependent Bcr-Abl degradation.MRLB-223 mediates p53-independent tumor cell death, with activity suppressed by Bcl-2 overexpression, and kills Bcr-Abl-expressing myeloid cells.MRLB-223 exerts effects in mice bearing Eμ-myc lymphomas.MRLB-223 can be used for the research of Eμ-myc lymphoma.

LSD1/HDAC-IN-1 (compound 2) is a potent inhibitor of HDAC and LSD1, with IC₅₀s of 0.125 nM, 0.373 nM, 0.0118 nM, 0.103 nM, and 0.571 μM for HDAC1, HDAC2, HDAC6, HDAC8 and LSD1, respectively. LSD1/HDAC-IN-1 plays an important role in cancer research.

HDAC-IN-27 (Compound 11h) is a potent, orally active class I HDAC-selective inhibitor with IC₅₀ values ranging from 0.43 to 3.01 nM against HDAC1-3. HDAC-IN-27 exhibits both in vivo and in vitro antitumor activity. HDAC-IN-27 demonstrates significant anti-proliferative activity against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). HDAC-IN-27 can be used for research in acute myeloid leukemia (AML).

CM-444 is inhibitor for HDAC (IC₅₀ is 6 nM-0.6 μM) and DNA methyltransferases (DNMT, IC₅₀ is 1.8-2.3 μM). CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models.

HDAC6-IN-74 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 0.036 μM. HDAC6-IN-74 induces tumor cell apoptosis, arrests cells at the S phase of the cell cycle, and impairs cell migration, invasion and colony-forming abilities. HDAC6-IN-74 exerts anticancer effects with no obvious toxicity. HDAC6-IN-74 can be used in the research of cancers such as liver cancer.

HDAC-IN-89 is an inhibitor of HDAC1 (IC₅₀: 0.95 nM), HDAC2 (IC₅₀: 0.86 nM), HDAC3 (IC₅₀: 1.06 nM) and HDAC8 (IC₅₀: 4.24 nM). HDAC-IN-89 blocks the cell cycle and induces apoptosis. HDAC-IN-89 has anti-tumor activity.

M122 is a potent inhibitor of HDAC1 and HDAC2, with the IC₅₀ values of 0.48 μM and 0.47 μM, respectively, respectively. M122 has antitumor activity.

PD-L1/HDAC-IN-1 (Compound 14) is the inhibitor for PD-L1 and HDAC that inhibits PD-1/PD-L1 interaction, HDAC2 and HDAC3 with IC₅₀ of 88.10, 27.98 and 14.47 nM, respectively. PD-L1/HDAC-IN-1 exhibits slight cytotoxicity in MCF-7 (IC₅₀=19.34 μM). PD-L1/HDAC-IN-1 upregulates the expression of PD-L1 and CXCL10, promoting anti-tumour immune response by recruiting T-cell infiltration into TME.

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].

BG47 is a prototypical histone deacetylases HDAC1 and HDAC2 selective, optoepigenetic probe. BG47 can bind to and competitively inhibits the deacetylase activity of HDAC targets upon a light-induced trans-to-cis isomerization, and increases Histone Methyltransferase H3K9 acetylation. BG47 can be used for neurological disease research.

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The K_i values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.