HDAC
Histone deacetylases
HDAC Isoform Specific Products
-
HDAC
(387)
View all products
-
HDAC1
(312)
View all products
-
HDAC2
(208)
View all products
-
HDAC3
(200)
View all products
-
HDAC4
(71)
View all products
-
HDAC5
(56)
View all products
-
HDAC6
(327)
View all products
-
HDAC7
(53)
View all products
-
HDAC8
(185)
View all products
-
HDAC9
(41)
View all products
-
HDAC10
(66)
View all products
-
HDAC11
(70)
View all products
-
HD1
(3)
View all products
-
HD2
(4)
View all products
All Product Categories
-
HDAC Inhibitors
(771)
View all products
-
HDAC Antagonists
(3)
View all products
-
HDAC Activators
(14)
View all products
-
HDAC Modulators
(4)
View all products
-
HDAC MDM2 Inhibitor
(1)
View all products
-
HDAC Degraders
(41)
View all products
-
HDAC Controls
(3)
View all products
-
HDAC Substrates
(3)
View all products
-
HDAC Ligands
(10)
View all products
-
HDAC Related Products (900)
Related Products (900)
-
Antibodies (16)
-
HDAC Signaling Pathway
-
HDAC Isoform Comparison
-
HDAC8-IN-17
0 ImagesCat. No.: HY-187382HDAC8-IN-17 is a histone deacetylase 8 inhibitor with human IC50 values of 0.08 μM, 0.44 μM, and 1.9 μM, and high selectivity over HDAC1, HDAC2, HDAC3, and HDAC6. HDAC8-IN-17 exhibits slow-binding, reversible uncompetitive inhibition via allosteric binding to the enzyme-substrate complex. HDAC8-IN-17 induces selective hyperacetylation of SMC3. HDAC8-IN-17 can be used for the research of cancer. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
HDAC6/HSP90-IN-1
0 ImagesCat. No.: HY-146293CAS No.: 2411955-43-4HDAC6/HSP90-IN-1 (compound 17) is a potent and selective dual inhibitor of HDAC6 and HSP90, with IC50 values of 4.3 and 46.8 nM, respectively. HDAC6/HSP90-IN-1 down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells. HDAC6/HSP90-IN-1 inhibits tumor growth in human H1975 xenograft mice. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
- HDAC8 ligand 1
-
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
HDAC6-IN-63
0 ImagesCat. No.: HY-178022HDAC6-IN-63 (Compound 7) is an orally active HDAC6 inhibitor with an IC50 of 145 nM. HDAC6-IN-63 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC6-IN-63 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC6-IN-63 can be used for chemotherapy of cancers like NSCLC research. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
Largazole thiol
0 ImagesCat. No.: HY-170890CAS No.: 1132667-11-8 -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
- HDAC6-IN-57
-
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
XP5
0 ImagesCat. No.: HY-115885CAS No.: 2760511-91-7XP5 is a potent, orally active HDAC6 inhibitor with an IC50 of 31 nM. XP5 displays high antiproliferative activity against various cancer cell lines including the HDACi-resistant YCC3/7 gastric cancer cells (IC50=0.16-2.31 μM). XP5 enhances antitumor immunity when combined with a PD-L1 inhibitor in melanoma. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
- HDAC6/HSP90-IN-3
-
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
IMPDH II/HDAC1-IN-1
0 ImagesCat. No.: HY-174221IMPDH II/HDAC1-IN-1 (Compound C12) is an orally active, selective dual IMPDH II/HDAC1 inhibitor, with an IC50 of 84.69 nM against hIMPDH II and an IC50 of 81.75 nM against HDAC1. IMPDH II/HDAC1-IN-1 inhibits the proliferation of chronic myeloid leukemia cells. IMPDH II/HDAC1-IN-1 can be used for the research of chronic myeloid leukemia. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
HDAC-IN-37
0 ImagesCat. No.: HY-146750CAS No.: 2766466-56-0 -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
- HDAC-IN-65
-
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
- c-Met/HDAC-IN-3
-
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
PARP-1/HDAC-IN-1
0 ImagesCat. No.: HY-146160CAS No.: 3032621-10-3PARP-1/HDAC-IN-1 is a PARP-1/HDAC6 dual targeting inhibitor with IC50s of 68.90 nM and 510 nM, respectively. PARP-1/HDAC-IN-1 displays remarkable anticancer, anti-migration and anti-angiogenesis activities. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
- HDAC6-IN-4
-
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
HDAC8-IN-12
0 ImagesCat. No.: HY-161954CAS No.: 3028095-13-5HDAC8-IN-12 (compound 5k) is a non-hydroxamic acid, selective inhibitor of HDAC8 (IC50: 0.12 nM) and a potent inhibitor of breast cancer. HDAC8-IN-12 triggers anti-tumor immunity by activating T cells, increasing the proportion of M1 macrophages and decreasing the proportion of M2 macrophages. HDAC8-IN-12 (50 mg/kg) exerts tumor suppressive effects in an orthotopic mouse model of breast cancer. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
CA/HDAC-IN-1
0 ImagesCat. No.: HY-179271CA/HDAC-IN-1 (Compound 11) is a CA and HDAC inhibitor with Ki values of 7.4 nM, 31.0 nM, and 7.3 nM for hCA II, hCA IX, and hCA XII, respectively, and IC50 values of 0.21 μM and 3.60 μM for HDAC3 and HDAC8, respectively. CA/HDAC-IN-1 has anti-cancer activity against colon cancer, breast cancer, and melanoma. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
HDAC6-IN-47
0 ImagesCat. No.: HY-163834HDAC6-IN-47 (Compound S-29b) is inhibitor for HDAC, which exhibits high affinities to HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, HDAC10 with Ki of 60, 56, 162, 0.44, 362 and 849 nM, respectively. HDAC6-IN-47 causes tubulin hyperacetylation in MV4-11, inhibits the proliferation of MV4-11 with an EC50 of 0.50 µM. HDAC6-IN-47 can be used in research of leukemia. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
PI3Kδ/HDAC6-IN-1
0 ImagesCat. No.: HY-174396CAS No.: 3075011-99-0PI3Kδ/HDAC6-IN-1 (Compound 22E) is an orally active and dual inhibitor of PI3Kδ and HDAC6 with IC50 values of 2.4 nM and 6.2 nM, respectively. PI3Kδ/HDAC6-IN-1 exhibits potent antiproliferative effects on non-Hodgkin lymphoma (NHL) cells and possesses in vivo antitumor activity without significant toxicity. PI3Kδ/HDAC6-IN-1 arrests the cell cycle at the G0/G1 phase and induces apoptosis. PI3Kδ/HDAC6-IN-1 blocks the PI3K/AKT/mTOR signaling pathway and increases the acetylation levels of α-tubulin and histone H3. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
GSK-3β/HDAC-IN-2
0 ImagesCat. No.: HY-174398GSK-3β/HDAC-IN-2 is a potent inhibitor of GSK-3β (IC50 = 0.04 μM), HDAC2 (IC50 = 1.05 μM, Ki = 0.070 μM) and HDAC6 (IC50 = 1.52 μM, Ki = 0.017 μM). GSK-3β/HDAC-IN-2 inhibits HDAC2 and HDAC6 activities and blocks tau hyperphosphorylation. GSK-3β/HDAC-IN-2 exerts neuroprotective effects and shows no significant toxicity. GSK-3β/HDAC-IN-2 can be used in the research of Alzheimer's disease. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
-
HDAC-IN-31
0 ImagesCat. No.: HY-144293CAS No.: 1916505-13-9HDAC-IN-31 is a potent, selective and orally active HDAC inhibitor with IC50s of 84.90, 168.0, 442.7, >10000 nM for HDAC1, HDAC2, HDAC3, HDAC8, respectively. HDAC-IN-31 induces apoptosis and cell cycle arrests at G2/M phase. HDAC-IN-31 shows good antitumor efficacy. HDAC-IN-31 has the potential for the research of diffuse large B-cell lymphoma. -
loading...Please select quantityGet Quote
August 31
-
Please select quantity
August 31
Get Quote
loading... -
No matching results
No matching results
No matching results
No matching results
No matching results
No matching results
No matching results
No matching results
No matching results
No matching results
TCR, GPCR and HDAC II interaction: Diverse agonists act through G-protein-coupled receptors (GPCRs) to activate the PKC-PKD axis, CaMK, Rho, or MHC binding to antigens stimulates TCR to activate PKD, leading to phosphorylation of class II HDACs. Phospho-HDACs dissociate from MEF2, bind 14-3-3, and are exported to the cytoplasm through a CRM1-dependent mechanism. CRM1 is inhibited by leptomycin B (LMB). Release of MEF2 from class II HDACs allows p300 to dock on MEF2 and stimulate gene expression. Dephosphorylation of class II HDACs in the cytoplasm enables reentry into the nucleus[1].
TLR: TLR signaling is initiated by ligand binding to receptors. The recruitment of TLR domain-containing adaptor protein MyD88 is repressed by HDAC6, whereas NF-κB and MTA-1 can be negatively regulated by HDAC1/2/3 and HDAC2, respectively. Acetylation by HATs enhance MKP-1 which inhibits p38-mediated inflammatory responses, while HDAC1/2/3 inhibits MKP-1 activity. HDAC1 and HDAC8 repress, whereas HDAC6 promotes, IRF function in response to viral challenge. HDAC11 inhibits IL-10 expression and HDAC1 and HDAC2 represses IFNγ-dependent activation of the CIITA transcription factor, thus affecting antigen presentation[2][3].
IRNAR: IFN-α/β induce activation of the type I IFN receptor and then bring the receptor-associated JAKs into proximity. JAK adds phosphates to the receptor. STATs bind to the phosphates and then phosphorylated by JAKs to form a dimer, leading to nuclear translocation and gene expression. HDACs positively regulate STATs and PZLF to promote antiviral responses and IFN-induced gene expression[2][3].
Cell cycle: In G1 phase, HDAC, Retinoblastoma protein (RB), E2F and polypeptide (DP) form a repressor complex. HDAC acts on surrounding chromatin, causing it to adopt a closed chromatin conformation, and transcription is repressed. Prior to the G1-S transition, phosphorylation of RB by CDKs dissociates the repressor complex. Transcription factors (TFs) gain access to their binding sites and, together with the now unmasked E2F activation domain. E2F is then free to activate transcription by contacting basal factors or by contacting histone acetyltransferases, such as CBP, that can alter chromatin structure[4].
The function of non-histone proteins is also regulated by HATs/HDACs. p53: HDAC1 impairs the function of p53. p53 is acetylated under conditions of stress or HDAC inhibition by its cofactor CREB binding protein (CBP) and the transcription of genes involved in differentiation is activated. HSP90: HSP90 is a chaperone that complexes with other chaperones, such as p23, to maintain correct conformational folding of its client proteins. HDAC6 deacetylates HSP90. Inhibition of HDAC6 would result in hyperacetylated HSP90, which would be unable to interact with its co-chaperones and properly lead to misfolded client proteins being targeted for degradation via the ubiquitin-proteasome system[5][6].
Reference:
[1]. Vega RB, et al. Protein kinases C and D mediate agonist-dependent cardiac hypertrophy through nuclear export of histone deacetylase 5.Mol Cell Biol. 2004 Oct;24(19):8374-85.
[2]. Shakespear MR, et al. Histone deacetylases as regulators of inflammation and immunity. Trends Immunol. 2011 Jul;32(7):335-43.
[3]. Suliman BA, et al. HDACi: molecular mechanisms and therapeutic implications in the innate immune system.Immunol Cell Biol. 2012 Jan;90(1):23-32.
[4]. Brehm A, et al. Retinoblastoma protein meets chromatin.Trends Biochem Sci. 1999 Apr;24(4):142-5.
[5]. Butler R, et al. Histone deacetylase inhibitors as therapeutics for polyglutamine disorders.Nat Rev Neurosci. 2006 Oct;7(10):784-96
[6]. Minucci S, et al. Histone deacetylase inhibitors and the promise of epigenetic (and more) treatments for cancer.Nat Rev Cancer. 2006 Jan;6(1):38-51.
Your Search Returned No Results.
Sorry. There is currently no product that acts on isoform Bcl-2, Bcl-W and Bim together.Please
try each isoform separately.