HDAC
Histone deacetylases (HDACs), known for their ability to target histones as well as more than 50 non-histone proteins, are classified into three major classes according to their homology to yeast proteins, including class I (HDAC1, HDAC2, HDAC3 and HDAC8), class II (HDAC4, HDAC5, HDAC7 and HDAC9) and class IV (HDAC11). HDAC inhibitors, a large group of compounds that is able to induce the accumulation of acetylated histones as well as non-histone proteins, are divided into several structural classes including hydroxamates, cyclic peptides, aliphatic acids and benzamides. HDAC inhibitors have been investigated for their efficacy as anticancer agents in the treatment of a wild range of cancers.
Products for HDAC
- Cat.No. Product Name Information
- GC39214 1-Naphthohydroxamic acid 1-Naphthohydroxamic acid (Compound 2) is a potent and selective HDAC8 inhibitor with an IC50 of 14 μM. 1-Naphthohydroxamic acid is more selectively for HDAC8 than class I HDAC1 and class II HDAC6 (IC50 >100 μM). 1-Naphthohydroxamic acid does not increase global histone H4 acetylation and also does not reduce total intracellular HDAC activity.1-Naphthohydroxamic acid can induce tubulin acetylation.
- GC11249 2-hexyl-4-Pentynoic Acid Potent and robust HDACs inhibitor
- GC17005 4-iodo-SAHA class I and class II histone deacetylase (HDAC) inhibitor
- GC12667 4SC-202 4SC-202 (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
- GC66055 5-Phenylpentan-2-one 5-Phenylpentan-2-one is a potent histone deacetylases (HDACs) inhibitor. 5-Phenylpentan-2-one can be used for urea cycle disorder research.
- GC48986 9-hydroxy Stearic Acid A hydroxy fatty acid
- GA20481 Ac-Arg-Gly-Lys(Ac)-AMC Ac-RGK(Ac)-AMC, fluorogenic substrate for assaying histone deacetylase (HDAC) activity in a two-step enzymatic reaction. The assay consists of the initial lysine deacetylation by HDAC followed by the release of the fluorescent group by trypsin.
- GA20605 Ac-Lys-AMC Ac-Lys-AMC is cleaved by trypsin.
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GC34458
ACY-1083
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.
- GC10417 ACY-241 ACY-241 (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). ACY-241 has anticancer effects.
- GC19020 ACY-738 ACY-738 is a potent, selective and orally-bioavailable HDAC6 inhibitor, with an IC50s of 1.7 nM; ACY-738 also inhibits HDAC1, HDAC2, and HDAC3, with IC50s of 94, 128, and 218 nM.
- GC30782 ACY-775 An HDAC6 inhibitor
- GC30526 ACY-957 ACY-957 is an orally active and selective inhibitor of HDAC1 and HDAC2, with IC50s of 7 nM, 18 nM, and 1300 nM against HDAC1/2/3, respectively, and shows no inhibition on HDAC4/5/6/7/8/9.
- GC65330 AES-135 AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC50s ranging from 190-1100 nM.
- GC48775 AES-350 An inhibitor of class I and class IIb HDACs
- GC49393 all-trans-13,14-Dihydroretinol A metabolite of all-trans retinoic acid
- GC67984 Alteminostat
- GC40674 APHA Compound 8 A class I and II HDAC inhibitor
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GC12961
Apicidin
A cell-permeable HDAC inhibitor
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GC14590
AR-42 (OSU-HDAC42)
HDAC inhibitor,novel and potent
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GC15962
Belinostat (PXD101)
Belinostat is an effective HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
- GC30763 Benzenebutyric acid (4-Phenylbutyric acid) Benzenebutyric acid (4-Phenylbutyric acid) (4-PBA) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
- GC12074 BG45 Novel HDAC3-selective inhibitor
- GC25139 Biphenyl-4-sulfonyl chloride Biphenyl-4-sulfonyl chloride (p-Phenylbenzenesulfonyl, 4-Phenylbenzenesulfonyl, p-Biphenylsulfonyl) is a HDAC inhibitor with synthetic applications in palladium-catalyzed desulfitative C-arylation.
- GC12822 BML-210(CAY10433) BML-210(CAY10433) is a novel HDAC inhibitor, and its mechanism of action has not been characterized.
- GC13926 BMS-345541(free base) BMS-345541(free base) is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541(free base) binds at an allosteric site of IKK.
- GC33331 BRD 4354 BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
- GC35551 BRD 4354 ditrifluoroacetate BRD 4354 (ditrifluoroacetate) is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
- GC50322 BRD 9757 Potent and selective HDAC6 inhibitor
- GC38742 BRD-6929 An HDAC1 and HDAC2 inhibitor
- GC40923 BRD4884 BRD4884 is an HDAC inhibitor with IC50 values of 29 nM, 62 nM, and 1.09 μM for HDAC1, 2, and 3, respectively.
- GC13088 BRD6688 HDAC inhibitor
- GC12484 BRD73954 potent and selective HDAC inhibitor
- GC15410 Bufexamac COX inhibitor
- GC64761 Butyric acid-13C1
- GC43147 CAY10398 CAY10398 is an inhibitor of histone deacetylase (HDAC1) with an IC50 value of 10 μM.
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GC12971
CAY10603
potent and selective inhibitor of HDAC6
- GC43200 CAY10721 CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM).
- GC43201 CAY10722 CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM).
- GC49029 CAY17c An inhibitor of BRD4 and class I and class IIb HDACs
- GC14058 CBHA CBHA is a potent HDAC inhibitor, exhibiting ID50 values of 10 and 70 nM in vitro for HDAC1 and HDAC3, respectively. CBHA also induces apoptosis and suppresses tumor growth.
- GC35668 CG-200745 CG-200745 (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. CG-200745 inhibits deacetylation of histone H3 and tubulin. CG-200745 induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. CG-200745 enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-Fluorouracil (5-FU; ). CG-200745 induces apoptosis and has anti-tumour effects.
- GC39679 CG347B CG347B is a selective HDAC6 inhibitor, also involves in synthesis of other metalloenzyme inhibitors.
- GC11975 CHAPS
- GC64942 CHDI-390576 CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform.
- GC16042 Chidamide Chidamide (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
- GC45717 Chlamydocin An HDAC inhibitor
- GC13408 CI994 (Tacedinaline) An inhibitor of HDAC1, -2, and -3
- GC65426 CM-675 CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively.
- GC34165 Corin Corin is a dual inhibitor of histone lysine specific demethylase (LSD1) and histone deacetylase (HDAC), with a Ki(inact) of 110 nM for LSD1 and an IC50 of 147 nM for HDAC1.
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GC43318
coumarin-SAHA
Suberoylanilide hydroxamic acid (SAHA) is a class I and class II histone deacetylase (HDAC) inhibitor that binds directly to the catalytic site of the enzyme thereby blocking substrate access.
- GC32565 CRA-026440 CRA-026440 is a potent, broad-spectrum HDAC inhibitor.
- GC67674 CRA-026440 hydrochloride
- GC38412 Crotonoside A guanosine analog with diverse biological activities
- GC16008 CUDC-101 A multi-target inhibitor of HDACs, EGFR, and HER2
- GC12115 CUDC-907 A dual inhibitor of HDACs and PI3Ks
- GC15830 Daminozide Selective inhibitor of KDM2/7 histone demethylases
- GC35893 Domatinostat Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
- GC13706 Droxinostat An inhibitor of HDAC3, HDAC6, and HDAC8
- GC19129 EDO-S101 EDO-S101 is a pan HDAC inhibitor; inhibits HDAC1, HDAC2 and HDAC3 with IC50 values of 9, 9 and 25 nM, respectively.
- GC64191 Elevenostat Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235??M). Anti-multiple myeloma (MM) activity.
- GC11625 Entinostat (MS-275,SNDX-275) A histone deacetylase inhibitor
- GC62461 FNDR-20123 FNDR-20123 is a safe, first-in-class, and orally active anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively.
- GC65206 FT895 FT895 is a potent and selective HDAC11 inhibitor with an IC50 of 3 nM.
- GC33050 Givinostat (ITF-2357) Givinostat (ITF-2357) (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
- GC33159 Givinostat hydrochloride (ITF-2357 hydrochloride) Givinostat (ITF-2357) hydrochloride is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
- GC18402 GSK3117391 GSK3117391 is a histone deacetylase (HDAC) inhibitor, extracted from patent WO/2008040934 A1.
- GC19190 HDAC-IN-4 HDAC-IN-4 is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. HDAC-IN-4 has no activity against HDAC class II. HDAC-IN-4 has antitumor activity.
- GC66052 HDAC-IN-40 HDAC-IN-40 is a potent alkoxyamide-based HDAC inhibitor with Ki values of 60 nM and 30 nM for HDAC2 and HDAC6, respectively. HDAC-IN-40 had antitumor effects.
- GC33395 HDAC-IN-5 HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor.
- GC41495 HDAC3 Inhibitor HDAC3 Inhibitor (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM.
- GC68010 HDAC3-IN-T247
- GC49693 HDAC5 (human, recombinant) Active, pure human recombinant enzyme
- GC41085 HDAC6 Inhibitor HDAC6 Inhibitor is a potent and selective HDAC6 inhibitor (IC50=36 nM). HDAC6 Inhibitor weakly inhibits other HDAC isoforms. HDAC6 Inhibitor inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
- GC33317 HDAC6-IN-1 HDAC6-IN-1 is a potent and selective inhibitor for HDAC6 with an IC50 of 17 nM and shows 25-fold and 200-fold selectivity relative to HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively.
- GC19189 HDAC8-IN-1 HDAC8-IN-1 is a HDAC8 inhibitor with an IC50 of 27.2 nM.
- GC65460 HDACs/mTOR Inhibitor 1 HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.
- GC12334 HNHA HDAC inhibitor
- GC11574 HPOB HDAC6 inhibitor, potent and selective
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GC17836
ITF2357 (Givinostat)
HDAC inhibitor with anti-inflammatory and antineoplastic activities
- GC14597 ITSA-1 (ITSA1) ITSA-1 (ITSA1) is an activator of histone deacetylase (HDAC), and counteract trichostatin A (TSA)-induced cell cycle arrest, histone acetylation, and transcriptional activation.
- GC63703 Ivaltinostat formic Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket.
- GC34629 J22352 J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC50 value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1.
- GC64959 JAK/HDAC-IN-1 JAK/HDAC-IN-1 is a potent JAK2/HDAC dual inhibitor, exhibits antiproliferative and proapoptotic activities in several hematological cell lines. JAK/HDAC-IN-1 shows IC50s of 4 and 2 nM for JAK2 and HDAC, respectively.
- GC15476 JNJ-26481585 A pan-HDAC inhibitor
- GC62430 KA2507 KA2507 is a potent, orally active and selective HDAC6 inhibitor, with an IC50 of 2.5 nM. KA2507 shows antitumor activities and immune modulatory effects in preclinical models.
- GC62374 KA2507 monohydrochloride KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities.
- GC13435 KD 5170 An inhibitor of class I and II HDACs
- GC25552 KT-531 KT-531 (KT531) is a potent, selective HDAC6 inhibitor with IC50 of 8.5 nM, displays 39-fold selectivity over other HDAC isoforms.
- GC15114 LAQ824 (NVP-LAQ824,Dacinostat) A hydroxamate-based HDAC inhibitor
- GC13237 LMK 235 A selective inhibitor of HDAC4 and HDAC5
- GC16456 M344 HDAC inhibitor
- GC61029 Marein A glucoside chalcone with diverse biological activities
- GC15965 MC1568 A selective class IIa HDAC inhibitor
- GC45906 MC1742 An inhibitor of class I and class IIb HDACs
- GC11949 MI-192 inhibitor of histone deacetylases (HDACs)
- GC13055 Mocetinostat (MGCD0103, MG0103) An orally available HDAC inhibitor
- GC64729 MPT0B390 MPT0B390 is an arylsulfonamide-based derivative with potent HDAC inhibitory ability. MPT0B390, TIMP3 inducer, inhibits tumor growth, metastasis and angiogenesis. MPT0B390 shows antiproliferative activity against human colon cancer cell line HCT116 with the GI50 of 0.03 μM.
- GC65965 MPT0E028 MPT0E028 is an orally active and selective HDAC inhibitor with IC50s of 53.0 nM, 106.2 nM, 29.5 nM for HDAC1, HDAC2 and HDAC6, respectively. MPT0E028 reduces the viability of B-cell lymphomas by inducing apoptosis and possesses potent direct Akt targeting ability and reduces Akt phosphorylation in B-cell lymphoma. MPT0E028 has good anticancer activity.
- GC62308 MPT0G211 MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291?nM).