Category: Endogenous Metabolite Apoptosis Inducers Other Apoptosis Bromodomain DNA Methyltransferase HDAC Histone Acetyltransferases Histone Demethylases Histone Methyltransferase JAK Histone Deacetylation Histones/Histone Peptides PDE EGFR HER2 DNA/RNA Synthesis mTOR PI3K HIV Bacterial Parasite Virus Protease Cell Cycle/Checkpoint Autophagy Mitophagy Notch Cancer Biology Neuroscience Apoptosis Adaptive Immunity Immunotherapeutics VD/VDR Toxins Natural Products Peptides Phytotoxins
- Cat.No. Product Name Information
- 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.
- 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.
- 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.
- GC19189 HDAC8-IN-1 HDAC8-IN-1 is a HDAC8 inhibitor with an IC50 of 27.2 nM.
HDAC inhibitor,novel and potent
- 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.
- 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.
- GC62434 LSD1/HDAC6-IN-1 LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM).
- GC36905 PI3K/HDAC-IN-1 PI3K/HDAC-IN-1 is a potent dual inhibitor of PI3K/HDAC, potently inhibits PI3Kδ and HDAC1 with IC50s of 8.1 nM and 1.4 nM, respectively.
- GC41495 HDAC3 Inhibitor HDAC3 Inhibitor (compound 5) is a potent and selective HDAC3 inhibitor, with an IC50 of 5.96 nM.
- GC12019 TCS HDAC6 20b TCS HDAC6 20b is a HDAC6-selective inhibitor. TCS HDAC6 20b blocks the growth of estrogen receptor α-positive breast cancer MCF-7 cells.
- GC33395 HDAC-IN-5 HDAC-IN-5 is a histone deacetylase (HDAC) inhibitor.
- gc21178 HDAC-IN-4 d4
- GC49693 HDAC5 (human, recombinant) Active, pure human recombinant enzyme
TH34 is a potent HDAC6/8/10 inhibitor
- GC13591 TC-H 106 TC-H 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs.
- GC13408 CI994 (Tacedinaline) CI994 (Tacedinaline) (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.
- GC17390 Vorinostat (SAHA, MK0683) Vorinostat (SAHA, MK0683) (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively.
- GC15526 Trichostatin A (TSA) Trichostatin A (TSA) (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
- GA20566 Ac-Gly-Ala-Lys(Ac)-AMC Ac-GAK(Ac)-AMC, fluorogenic substrate for measuring histone deacetylase class I (HDAC 1, 2, 3, and 8) and class II (HDAC 6 and 10) activity in a protease-coupled assay. HDAC-catalyzed deacetylation of Lys yields Ac-GAK-AMC (I-1980).
- GC64684 SB-429201 SB-429201 is a potent and selective HDAC1 (IC50~1.5 μM). SB-429201 displays at least a 20-fold preference for HDAC1 inhibition over HDAC3 and HDAC8.
- 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.
- GA21064 Boc-Lys(Tfa)-AMC Fluorogenic substrate for assaying histone deacetylase (HDAC) 4, 5 and 7 activity in a protease-coupled assay. Suitable substrate for HDAC 8. The deacylated product Boc-Lys-AMC corresponds to I-1880.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
- GC52166 NN-390 NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma).
- 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.
- 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.
- GC65254 MC4355 MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC).
- GC65206 FT895 FT895 is a potent and selective HDAC11 inhibitor with an IC50 of 3 nM.
- GC64968 SW-100 SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes.
- 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.
- 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.
- GC19936 Quisinostat dihydrochloride Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity.
- GC64378 Valproic acid-d6 Valproic acid-d6 (VPA-d6) is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
- GC64191 Elevenostat Elevenostat (JB3-22) is a selective HDAC11 inhibitor (IC50=0.235??M). Anti-multiple myeloma (MM) activity.
- GC63730 QTX125 TFA QTX125 TFA is a potent and highly selective HDAC6 inhibitor. QTX125 TFA exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects.
- 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.
- GC49029 CAY17c An inhibitor of BRD4 and class I and class IIb HDACs
- 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.
- GC62411 QTX125 QTX125 is a potent and highly selective HDAC6 inhibitor. QTX125 exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects.
- GC62374 KA2507 monohydrochloride KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities.
- GC62308 MPT0G211 MPT0G211 is a potent, orally active and selective HDAC6 inhibitor (IC50=0.291?nM).
- GC61947 Triciferol Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.
- GC48775 AES-350 An inhibitor of class I and class IIb HDACs
- GC48460 NR-160 An inhibitor of HDAC6
- GC48408 TW9 A dual inhibitor of BRD4 and HDAC1
- GC48084 Sodium 4-Phenylbutyrate-d11 Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
- GC60310 Psammaplin A Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases.
- GC39679 CG347B CG347B is a selective HDAC6 inhibitor, also involves in synthesis of other metalloenzyme inhibitors.
- GC39551 BRD3308 BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM.
- GC50322 BRD 9757 Potent and selective HDAC6 inhibitor
- 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.
- GC46226 SS-208 An HDAC6 inhibitor
- GC38742 BRD-6929 An HDAC1 and HDAC2 inhibitor
- GC45906 MC1742 An inhibitor of class I and class IIb HDACs
- GC45717 Chlamydocin An HDAC inhibitor
- GA21261 Checkpoint Protein Hus1 (213-232) (human) HDAC1 plays an important role in modulating the eukaryotic chromatin structure and was found to interact specifically in yeast, mammalian cells, and in vitro with the human Hus1 gene product, as reported by Cai and coworkers. The Hus1 protein of S. pombe has been implicated in G2/M checkpoint control and is a member of the cell cycle checkpoint Rad proteins that are involved in the mitotic checkpoint induced by either DNA damage or DNA replication block.
- GA20567 Ac-Gly-Ala-Lys-AMC Ac-GAK-AMC, control peptide for protease-coupled histone deacetylase (HDAC) assay with Ac-Gly-Ala-Lys(Ac)-AMC (I-1975).
- GC37845 Tucidinostat An HDAC inhibitor
- GC37753 Tefinostat Tefinostat (CHR-2845) is a monocyte/macrophage targeted histone deacetylase (HDAC) inhibitor. Tefinostat can be cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Tefinostat can be used for the research of leukaemias.
- GC37643 SIS17 SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
- GC36691 Nanatinostat Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM.
- GC36690 Nampt-IN-3 Nampt-IN-3 (Compound 35) simultaneously inhibit nicotinamide phosphoribosyltransferase (NAMPT) and HDAC with IC50s of 31 nM and 55 nM, respectively. Nampt-IN-3 effectively induces cell apoptosis and autophagy and ultimately leads to cell death.
- 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).
- 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.
- 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.
- GC45095 Tubastatin A (trifluoroacetate salt) Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM.
- GC44865 SAHA-BPyne 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.
- GC43806 HC Toxin HC Toxin is a cell-permeable, reversible inhibitor of histone deacetylases (HDACs) (IC50 = 30 nM).
- GC43460 Dihydrochlamydocin Dihydrochlamydocin is a cyclic tetrapeptide with putative histone deacetylase (HDAC) inhibitory activity.
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.
- GC43201 CAY10722 CAY10722 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (71% inhibition at 200 μM).
- GC43200 CAY10721 CAY10721 is an inhibitor of sirtuin 3 (SIRT3), a class III HDAC (39% SIRT3 inhibition at 200 μM).
- GC43147 CAY10398 CAY10398 is an inhibitor of histone deacetylase (HDAC1) with an IC50 value of 10 μM.
- GC41984 1-Alaninechlamydocin 1-Alaninechalmydocin is a fungal metabolite originally isolated from a Great Lakes-derived Tolypocladium sp.
- 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.
- GC40674 APHA Compound 8 A class I and II HDAC inhibitor
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.
- 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.
- GC33331 BRD 4354 BRD 4354 is a moderately potent inhibitor of HDAC5 and HDAC9, with IC50s of 0.85 and 1.88 μM, respectively.
- GC33290 Remetinostat (SHP-141) Remetinostat (SHP-141) (SHP-141) is a hydroxamic acid-based inhibitor of histone deacetylase enzymes (HDAC) which is under development for the treatment of cutaneous T-cell lymphoma.
- 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.
- GC33115 Pomiferin (NSC 5113) Pomiferin (NSC 5113) (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).
- 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.
- GC32964 NKL 22 A selective HDAC1/3 inhibitor
- GC32565 CRA-026440 CRA-026440 is a potent, broad-spectrum HDAC inhibitor.
- GC30782 ACY-775 An HDAC6 inhibitor
- 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.
- GC30616 3-Hydroxybutyric acid An endogenous and specific inhibitor of class I HDACs
An alkylatlng histone-deacetylase inhibitor (HDACi) fusion molecule
- GC19384 WT-161 WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM.
- GC19360 TMP195 TMP195 is a potent and selective class IIa HDAC inhibitor with IC50s of 59 nM, 60 nM, 26 nM and 15 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
- GC19337 SR-4370 SR-4370 is an inhibitor of HDAC, with IC50s of 0.13 uM, 0.58 uM, 0.006 uM, 2.3 uM, and 3.4 uM for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, respectively.
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