HDAC|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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HDAC (Histone deacetylases) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on ahistone, allowing the histones to wrap the DNA more tightly. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone acetyltransferase. HDAC proteins are now also called lysine deacetylases (KDAC), to describe their function rather than their target, which also includes non-histone proteins. Together with the acetylpolyamine amidohydrolases and the acetoin utilization proteins, the histone deacetylases form an ancient protein superfamily known as the histone deacetylase superfamily.

Cat. No.	Product Name	CAS No.	Information
H9629	KT-531	2490284-18-7	KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms;KT-531 demonstrated biological potency in multiple hematological cancer cell models (acute myeloid leukemia (AML), PTCL, and T-cell acute lymphoblastic leukemia (T-ALL)) and limited cytotoxicity in nonmalignant cell types as well as no observable toxicity in vivo (CD-1 mice).KT-531 exhibited strong potency (IC50=0.42 μM) in the T-ALL/T-PLL-like cell line SUP-T11, demonstrated higher cytotoxicity than Nexturastat in MV4-11 cancer cells (IC50=0.42 uM versus 1.68 uM).KT-531 showed high synergy with chemotherapeutic agents idasanutlin, bendamustine, and venetoclax in T-PLL patient samples.KT-531 is the first HDAC6 inhibitor to show efficacy in T-PLL patient samples.
H9389	Pomiferin	572-03-2	Pomiferin (NSC 5113) acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
H8745	Ivaltinostat	936221-33-9	Ivaltinostat is a novel hydroxamate-based pan-histone deacetylase inhibitor (HDACI). Like other inhibitors, CG200745 has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket; CG200745 inhibited deacetylation of histone H3 and tubulin as much as vorinostat and belinostat did. CG200745 also inhibited growth of prostate cancer cells, increased sub-G1 population, and activated caspase-9, -3 and -8 in LNCaP, DU145 and PC3 cells.
H2637	WT-161	1206731-57-8	A potent, selective, and bioavailable HDAC6 inhibitor with IC50 0.4 nM; displays >20-fold selectivity over HDAC1/2/3/8; selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin with little effect on global lysine acetylation in cells; reversibly and rapidly induces the accumulation of Ac-α-tubulin in MM cell lines, displays synergism with both BTZ and CFZ, caspase activation and apoptosis; demonstrates a significant antitumor effect in human MM cell xenograft mouse model combined with BTZ.
H2636	Vorinostat	149647-78-9	A potent HDAC inhibitor, inhibits the activities of HDAC1 and HDAC3 with IC50 of 10 nM and 20 nM, respectively; inhibits cell growth, induce terminal differentiation and prevent the formation of tumours in mice models.
H2635	Valproic acid sodium salt	1069-66-5	A HDAC inhibitor that selectively inhibits the catalytic activity of class I HDACs, and induces proteasomal degradation of HDAC2; induces differentiation of carcinoma cells, transformed hematopoietic progenitor cells and leukemic blasts from AML patients; reduces tumor growth and metastasis formation in animal model.
H2634	Valproic acid	99-66-1	A HDAC inhibitor that selectively inhibits the catalytic activity of class I HDACs, and induces proteasomal degradation of HDAC2; induces differentiation of carcinoma cells, transformed hematopoietic progenitor cells and leukemic blasts from AML patients; reduces tumor growth and metastasis formation in animal model.
H2633	UF-010	537672-41-6	A potent and selective inhibitor of class I HDACs with IC50s of 0.5/0.1/0.06/1.5/9.1/15.3/44.5 uM for HDAC1/2/3/8/6/10/11 respectively; shows no effect on HDAC4/5/7/9(>100 uM); induces the accumulation of protein acetylation and inhibits proliferation of NCI-60 panel of cancer cell lines (mean GI50=2.94 uM); a competitive with a fast-on/slow-off HDAC-binding mechanism.
H2632	Tucidinostat	1616493-44-7	Tucidinostat (Chidamide, HBI-8000, CS055) is a novel histone deacetylase (HDAC) inhibitor with IC50 of 95/160/67/733/78/432 nM for HDAC1/2/3/8/10/11, respectively; shows no activity against Class IIa HDAC4/4/7/9 and HDAC6; demonstrates significant and broad spectrum in vitro and in vivo antitumor activity, induces G1 arrest, ROS-dependent apoptosis and differentiation in human leukaemia cells.
H2631	Tubastatin A hydrochloride	1310693-92-5	Tubastatin A hydrochloride is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in cell-free assays; displays 57-fold selectivity over HDAC8 and >1,000-fold selective against other HDAC isoforms; induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines at 10 uM, shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with IC50 of 272 nM and 712 nM; reduces the growth of cholangiocarcinoma in vivo.

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