Signaling Pathway

HDAC

HDAC

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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. Types: HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, HDAC9, HDAC10, HDAC11.

HDAC Inhibitors & Modulators (59)

Product Name Catalog No. Brief Description
4SC-202

HY-16012

4SC-202 is an orally available potent HDACi specific for class I HDAC isoenzymes(NO HDAC8) with IC50s of 1.2/1.12/0.57 uM for HDAC1/2/3; high selectivity over ClassIIa/IIb/III HDACs.

4SC-202 free base

HY-16012A

4SC-202 free base is an orally available potent HDACi specific for class I HDAC isoenzymes(NO HDAC8) with IC50s of 1.2/1.12/0.57 uM for HDAC1/2/3; high selectivity over ClassIIa/IIb/III HDACs.

ACY-1215

HY-16026

Rocilinostat (ACY-1215) is a selective HDAC6 inhibitor with IC50 of 5 nM; >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2.

ACY-738

HY-19327

ACY-738 demonstrates inhibitory activity against recombinant HDAC6 with IC50 values of 1.7 nM, with respective average selectivity over class I HDACs being 100-fold.

Belinostat

HY-10225

Belinostat (PXD101) is a novel pan-HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors.

BG45

HY-18712

BG45 is an HDAC class I inhibitor with selectivity for HDAC3 (IC50 = 289 nM).

BML-210

HY-19350

BML-210 is the novel HDAC inhibitor, and its mechanism of action has not been characterized.

BRD73954

HY-18700

BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.

CAY10603

HY-18613

CAY10603 is a potent and selective inhibitor of HDAC6 with IC50 of 2 pM, as compared with 271, 252, 0.42, 6851, and 90.7 nM for HDAC1, 2, 3, 8, and 10, respectively.

Chidamide

HY-13592

Chidamide(CS055; HBI-8000) is a class I HDAC inhibitor with IC50s of 95/160/67/733 nM for HDAC1/2/3/8; also inhibits HDAC10/11(IC50=78/432 nM); no inhibition on HDAC4/5/7/9/6(IC50>30 uM).

CI-994

HY-50934

CI-994 (Tacedinaline) is an anti-cancer drug which inhibits HDAC1 with IC50 of 0.57 μM and causes G1 cell cycle arrest.

CUDC-101

HY-10223

CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively.

CUDC-907

HY-13522

CUDC-907 potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes.

Dacinostat

HY-13606

Dacinostat (NVP-LAQ824, LAQ824) is a highly potent HDAC inhibitor with IC50 of  32 nM.

Droxinostat

HY-13267

Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.

Entinostat

HY-12163

Entinostat (MS-275; SNDX 275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM.

Givinostat

HY-14842

Givinostat (ITF-2357) is a potent HDAC inhibitor for Maize HD2, HD1-B and HD1-A with IC50 of 10 nM, 7.5 nM and 16 nM,respectively.

Givinostat hydrochloride

HY-14842A

Givinostat (ITF-2357) hydrochloride is a potent HDAC inhibitor for Maize HD2, HD1-B and HD1-A with IC50 of 10 nM, 7.5 nM and 16 nM, respectively.

HDAC-IN-1

HY-15140

HDAC-IN-1 is a chemical analog of MC 1568, which is a potent and selective class IIa HDACs inhibitor.

HDAC-IN-2

HY-15994

HDAC-IN-2 is a HDAC6 specific inhibitor, with IC50 of 4 nM and 76 nM for HDAC6 and HDAC3, respectively.