HDAC Inhibitor

HDAC/CK2-IN-1 (compound 38) is a HDAC1 (IC₅₀ = 1.46 μM), HDAC6 (IC₅₀ = 0.66 μM), and CK2 (IC₅₀ = 3.67 μM) inhibitor. HDAC/CK2-IN-1 exhibits promising antproliferative activity against Jurkat, MCF-7, HCT-116, and HL-60 cell lines.

ZYJ-34v is an orally active histone deacetylase inhibitor. ZYJ-34v has antitumor activity.

HDAC-IN-54 is a HDAC inhibitor with an IC₅₀ of 25 nM against human HDAC1, 66 nM against HDAC2, 6.5 nM against HDAC3, and 281 nM against HDAC6. HDAC-IN-54 induces acetylation of α-tubulin and histone H3. HDAC-IN-54 acts synergistically with cisplatin to induce cancer cell apoptosis. HDAC-IN-54 can be used in research related to head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma.

HDAC-IN-34 (compound 27) is a potent HDAC inhibitor, with IC₅₀ values of 0.022 and 0.45 μM for HDAC1 and HDAC6, respectively. HDAC-IN-34 can bind to DNA and cause DNA damage. HDAC-IN-34 causes cells apoptosis through p53 signaling pathway. HDAC-IN-34 exhibits significant anti-proliferation effect against HCT-116 cells, with an IC₅₀ of 1.41 μM.

DNA-PK/HDAC6-IN-2 is an orally active and selective dual-target inhibitor of DNA-PK and HDAC6, with an IC₅₀ of 34.22 nM for DNA-PK and an IC₅₀ of 241.2 nM for HDAC6. DNA-PK/HDAC6-IN-2 upregulates Ac‑α‑tubulin, inhibits p‑DNA‑PK, and increases γ‑H2AX. DNA-PK/HDAC6-IN-2 exhibits antiproliferative activity against multiple solid tumor cell lines, induces apoptosis and cell cycle arrest, and inhibits migration and invasion. DNA-PK/HDAC6-IN-2 has in vivo antitumor efficacy in melanoma and breast cancer models and enhances the efficacy of Doxorubicin (HY-15142A). DNA-PK/HDAC6-IN-2 can be used for research on various cancers such as melanoma, breast cancer, and colorectal cancer.

Vorinostat (GMP) is a GMP grade Vorinosta (HY-10221). GMP-grade small molecules can be used as auxiliary agents in cell therapy. Vorinostat is a potent, orally available HDAC1, HDAC2, HDAC3 (Class I), HDAC6 and Inhibitors of HDAC7 (Class II) and Class IV (HDAC11).

HDAC6-IN-76 (Compound G25) is a selective HDAC6 inhibitor with an IC₅₀ of 12 nM. HDAC6-IN-76 induces Autophagy in a p53-dependent manner. HDAC6-IN-76 induces Apoptosis in a p53-dependent manner. HDAC6-IN-76 exhibits anticancer activity against hematologic malignancies, including acute myeloid leukemia.

A2AAR/HDAC-IN-2 is a potent A_2AAR/HDAC dual inhibitor, with good binding affinity for A_2AAR (K_i=10.3 nM) and good inhibitory activity against HDAC1 (IC₅₀=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor.

JN210 is a dual inhibitor of DCN1 and HDAC, with an IC₅₀ of 94.26 nM against human DCN1. JN210 disrupts the UBE2M-DCN1 protein-protein interaction, blocks the neddylation modification of cullin-RING ligases, inhibits HDAC activity and induces histone hyperacetylation. JN210 impairs DNA damage repair function, induces cell apoptosis, exerts cytotoxicity and inhibits tumor growth. JN210 can be used for the research of non-small cell lung cancer.

HDAC-IN-49 is a potent unselective HDAC (HDAC) inhibitor with IC₅₀s of 13 nM, 14 nM, 21 nM, 1880 nM, and 10 nM for HDAC1, HDAC2, HDAC3, HDAC4, and HDAC6. HDAC-IN-49 demonstrates prominent antileukemic activity with low cytotoxic activity toward healthy cells.

HDAC1-IN-5 is a potent HDAC1 inhibitor with IC₅₀ values of 15 nM and 20 nM for HDAC1 and HDAC6, respectively. HDAC1-IN-5 can enhance the acetylation of histone H3 and α-tubulin, as well as promote the activation of caspase 3 in cancer cells, thereby inducing apoptosis. HDAC1-IN-5 induces chromatin damage by binding with DNA. HDAC1-IN-5 has strong inhibitory activity against tumor growth in xenograft mice.

HDAC6-IN-60 (Compound 12) is an orally active and selective HDAC6 inhibitor. HDAC6-IN-60 exerts effects on tumor cell proliferation by inhibiting the enzymatic activity of HDAC6 and regulating pathways related to protein homeostasis. HDAC6-IN-60 is promising for research of HDAC6- related cancers.

anti-TNBC agent-12 (Compound 23a) is a multi-target antitumor agent targeting HDAC6 (IC₅₀=30.3 nM), DNA, and inducing nitric oxide (NO) release. anti-TNBC agent-12 induces tumor cell apoptosis and G2/M phase cell cycle arrest. anti-TNBC agent-12 is promising for research of triple-negative breast cancer (TNBC).

IHCH-3185 is an orally active class I HDAC inhibitor (HDAC1 IC₅₀ =102.9 nM) and A_2AR antagonist (A_2AR K_i =7.6 nM). IHCH-3185 reverses immune gene silencing by inducing histone acetylation and blocks the adenosine signaling pathway to relieve T-cell suppression. IHCH-3185 exhibits antiproliferative activity, induces cell cycle arrest, and significantly improves the tumor microenvironment. IHCH-3185 reduces the proportion of regulatory T cells, increases the CD8⁺/T_reg ratio, and upregulates the expression of key factors such as H2-K1, Cxcl9 and Cxcl10. IHCH-3185 shows significant antitumor potential in CT26 and MC38 mouse tumor models and is suitable for related cancer research.

HDAC6-IN-29 (compound 11g), hydroxamic analogue, is a HDAC6 inhibitor. HDAC6-IN-29 has potent antiproliferative activity against CAL-51 cells (IC₅₀ = 1.17 μM) and is able to induce apoptosis and cause accumulation of cells in the S phase of the cell cycle. HDAC6-IN-29 can be used for the research of cancer.

HDAC6-IN-59 (Compound 38k) is a highly selective histone deacetylase 6 (HDAC6) inhibitor (IC₅₀=3.12 nM, with 352-fold selectivity over HDAC1). HDAC6-IN-59 is promising for research of esophageal cancer.

HDAC-IN-33 is a potent HDAC inhibitor with IC₅₀s of 24, 46, and 47 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-33 possesses potent antiproliferation activities against tumor cells. HDAC-IN-33 shows potent antitumor efficacy in vivo That trigger antitumor immunity.

HDAC2-IN-3 is a selective, orally active, blood-brain barrier permeable HDAC2 inhibitor with an IC₅₀ of 14 nM. HDAC2-IN-3 upregulates histone acetylation levels in cells and in vivo, and enhances long-term potentiation (LTP) in the hippocampus. HDAC2-IN-3 can be used for the research of Alzheimer's disease.

HDAC6-IN-43 (compound 26) is a potent HDAC inhibitor. HDAC6-IN-43 effectively inhibits several HDACs, notably HDAC1, HDAC2, and HDAC6 (IC₅₀ < 150 nM), displaying a particularly high sensitivity towards HDAC6 (IC₅₀ = 11 nM). HDAC6-IN-43 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD).

HDAC-IN-93 is a HDAC inhibitor with promising total pan-HDAC inhibitory activity. HDAC-IN-93 demonstrates significant broad-spectrum antiproliferative activity across various cancer cell lines. HDAC-IN-93 induces cell apoptosis along with necrosis. HDAC-IN-93 can be used for the studies of prostate cancer and breast cancer.