HDAC8 Inhibitor

HDAC8-IN-15 is a selective HDAC8 inhibitor with an IC₅₀ of 0.40 μM. HDAC8-IN-15 increases the acetylation level of the HDAC8 substrate SMC3 without altering the total protein level of SMC3. HDAC8-IN-15 reduces cancer cell viability, inhibits colony formation, slows cell migration, induces apoptosis, and causes cell cycle arrest at the SubG1 phase. HDAC8-IN-15 can be used in studies related to neuroblastoma.

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.

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.

HDAC8-IN-14, a curcuminoid derivative, is a selective HDAC8 inhibitor with a Ki of 9 nM. HDAC8-IN-14 induces the production of reactive oxygen species (ROS), disrupts mitochondrial membrane potential, and promotes apoptosis. HDAC8-IN-14 can significantly promote the accumulation of cells in the sub-G0/G1 phase, consistent with apoptotic or necrotic cell death. HDAC8-IN-14 induces upregulation of cytochrome c, cleaved caspase-3, and the pro-apoptotic protein Bak while leaving the anti-apoptotic Bcl-2 levels unaltered. HDAC8-IN-14 can be used for the study of leukemia.

HYF031 is a selective, blood-brain barrier-permeable HDAC8 inhibitor with an IC₅₀ of 5.7 nM, and exhibits extremely low activity against most other HDAC subtypes. HYF031 is applicable for HDAC8 imaging studies.

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.

ZYJ-34c is an orally active and potent histone deacetylase inhibitor (HDACi) with IC₅₀s of 0.056 μM and 0.146 μM for HDAC6 and HDAC8, respectively. ZYJ-34c causes G1 phase arrest in low concentration. ZYJ-34c has antiproliferative activities. ZYJ-34c exhibits antitumor potency in MDA-MB-231 and HCT116 xenograft models and possesses antimetastatic potential in a mouse hepatoma-22 (H22) pulmonary metastasis model.

HDAC1-IN-15 is a HDAC1 inhibitor with activity against hHDAC1, PfHDAC1 and HDAC8. HDAC1-IN-15 inhibits the proliferation of asexual blood-stage Plasmodium falciparum and reduces the survival rate of stage IV-V gametocytes of Plasmodium falciparum. HDAC1-IN-15 is applicable to malaria-related research.

(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.

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.

J1075 is a selective Schistosoma mansoni HDAC8 inhibitor (with decreased affinity for human HDAC8). J1075 can induce apoptosis (Apoptosis) and death in schistosome cells. J1075 holds research value in the field of anti-parasitic agents.

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.

ZYJ-25e is a potent histone deacetylase inhibitor (HDACi) with IC₅₀s of 0.047 μM and 0.139 μM for HDAC6 and HDAC8, respectively. ZYJ-25e is a tetrahydroisoquinoline-bearing hydroxamic acid analogue. ZYJ-25e shows marked antitumor potency in the MDA-MB231 xenograft model.