HDAC Inhibitor

Hdac10 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Hdac10 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

HDAC3/BRD4-IN-1 (compound 26n) is an inhibitor of HDAC3/BRD4 with an IC₅₀ of 8 nM for HDAC3 (IC₅₀s are 220 nM and 120 nM for HDAC1 and HDAC2, respectively). HDAC3/BRD4-IN-1 has anti-tumor and anti-proliferative effects by upregulating Ac-H3 and downregulating c-Myc. The half-life of HDAC3/BRD4-IN-1 in human liver microsomes is 29.36 min.

YKL-05-093 is a salt-induced kinase (SIK) inhibitor (SIK2: K_d = 7.1 nM). YKL-05-093 reduces the phosphorylation level of HDAC4/5/CRTC2, inhibits SOST expression, and stimulates RANKL expression in vitro and in vivo. YKL-05-093 can be used in research on bone diseases.

PySAHA is a multifunctional HDAC inhibitor. PySAHA can degrade intracellular HDAC via a hydrophobic tagging mechanism. PySAHA also possesses photodynamic therapeutic activity and can generate reactive oxygen species under light irradiation. PySAHA can inhibit the proliferation, migration and induce cell apoptosis of breast cancer cells. PySAHA has antitumor activity and can be used in breast cancer research.

HDAC6-IN-30 (compound 8g) is a selective HDAC6 inhibitor with the IC₅₀ 21 nM, and increase cell protein acetylation levels.

HDAC-IN-32 is a potent HDAC inhibitor with IC₅₀s of 5.2, 11, and 28 nM for HDAC1, HDAC2 and HDAC6, respectively. HDAC-IN-32 possesses potent antiproliferation activities against tumor cells. HDAC-IN-32 shows potent antitumor efficacy in vivo That trigger antitumor immunity.

HDAC/NAMPT-IN-1 (compound 39h) is a dual inhibitor of HDAC and NAMPT with IC₅₀ values of 0.72-37081 nM and 1618 nM.

HDAC-IN-77 (HL-5s) is an HDAC inhibitor. HDAC-IN-77 can induce ferroptosis and inhibit the Nrf2/HO-1 signaling pathway. HDAC-IN-77 can be used in cancer research.

HDAC-IN-85 (Compound 1) is a BBB-permeable HDAC inhibitor. HDAC-IN-85 has an inhibitory effect on brain tumor cell lines. HDAC-IN-85 can induce acetylation, leading to DNA double-strand breaks, and induce the ubiquitination of RAD51, disrupting the DNA repair process. HDAC-IN-85 can be used in the research of glioblastoma.

HDAC6-IN-19 (Compound 14g) is a HDAC6 inhibitor (IC₅₀: 2.68 nM). HDAC6-IN-19 also inhibits HDAC1, HDAC2 and HDAC3 with IC₅₀s of 61.6 nM, 98.7 nM and 103 nM. HDAC6-IN-19 potently inhibits multiple cancer cell proliferation, including leukemia, colon cancer, melanoma, and breast cancer cell lines.

PD-L1/HDAC3-IN-1 (PH3) is a dual PD-L1/HDAC3 Inhibitor with IC₅₀ values of 89.4 nM and 107 nM for PD-1/PD-L1 and HDAC3, respectively. PD-L1/HDAC3-IN-1 induces cell apoptosis and arrests cell cycle at G0/G1 phase. PD-L1/HDAC3-IN-1 shows anticancer activity both in vivo and in vitro.

NCT-14b is a HDAC6-selective inhibitor. NCT-14b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells.

PARP/HDAC-IN-1 (compound B102) is a potent dual inhibitor of PARP and HDAC. PARP/HDAC-IN-1 inhibits PARP1, PARP2 and HDAC1 with IC₅₀s of 19.01, 2.13, 1690 nM, respectively.

Topo II/HDAC-IN-1 (7d) exhibits excellent dual inhibitory activities against Topo II and HDAC. Topo II/HDAC-IN-1 (8d) induces apoptosis.

GK444 (Compound 15a) is a HDAC1/2 inhibitor (IC₅₀: 100 and 92 nM for HDAC1/2 respectively). GK444 inhibits Caco-2 cells with IC₅₀ of 4.1 μM. GK444 also reduces TGF-β1 induced COL1A1 mRNA levels in primary normal human lung fibroblasts. GK444 inhibits Bleomycin (HY-108345)-induced lung fibrosis in mice.

HDAC-IN-44 is a HDAC inhibitor with the IC₅₀ value of 61.2 nM.
HDAC-IN-44 shows high anticancer activity towards multiple cancer cell lines.

Hdac10 Rat Pre-designed siRNA Set A contains three designed siRNAs for Hdac10 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

Sodium butyrate (GMP) refers to Sodium butyrate (HY-B0350A) of GMP grade. Small molecules of GMP grade can be used as adjuvants in cell therapy. Sodium Butyrate (sodium butanoate) is an inhibitor of HDAC, possessing anti-tumor activity.

HDAC-IN-60 (compound 21a) is a potent histone deacetylase (HDAC) inhibitor. HDAC-IN-60 can promote the intracellular generation of ROS, cause DNA damage, block the cell cycle at G2/M phase, and activate the mitochondria-related apoptotic pathway to induce cell apoptosis.

PI3K/HDAC-IN-3 (36) is a PI3K and HDAC dual inhibitor, with IC₅₀ values of 0.23 nM and 172 nM for PI3Kα and HDAC1, respectively. PI3K/HDAC-IN-3 (36) suppresses AKT phosphorylation and increased H3 acetylation in MV4-11 cells. PI3K/HDAC-IN-3 (36) exhibits significant and dose-dependent anticancer efficacy in a MV4-11 xenograft model.