HDAC1

HDAC1 is a class I histone deacetylase that supports transcriptional repression through histone deacetylase activity^[1]. Mechanistically, HDAC1/2 form core catalytic components of corepressor complexes that modulate gene expression, linking chromatin regulation to proliferation and stem-cell self-renewal^[2]. In human tumor cells, HDAC1 knockdown causes G₁ or G₂/M arrest, growth inhibition, loss of mitotic cells, and increased apoptosis^[3]. In embryonic stem cells, HDAC1, but not HDAC2, is required for optimal corepressor-complex activity and cell-fate determination during differentiation^[4]. Compared with HDAC2, HDAC1 shows nonredundant disease relevance in glioma stem cells, where its loss is not compensated by HDAC2 and affects the glioma stem-cell phenotype in a p53-dependent manner^[5]. For experimental applications, selective HDAC1/2 inhibition suppresses colorectal cancer cells through apoptosis induction and cell-cycle regulation, supporting inhibitor use in pathway-focused cancer models^[6].

References:

[1]. Hassig CA, et al. A role for histone deacetylase activity in HDAC1-mediated transcriptional repression. Proc Natl Acad Sci U S A. 1998 Mar 31;95(7):3519-24.

[2]. Jamaladdin S, et al. Histone deacetylase (HDAC) 1 and 2 are essential for accurate cell division and the pluripotency of embryonic stem cells. Proc Natl Acad Sci U S A. 2014 Jul 8;111(27):9840-5.

[3]. Senese S, et al. Role for histone deacetylase 1 in human tumor cell proliferation. Mol Cell Biol. 2007 Jul;27(13):4784-95.

[4]. Dovey OM, et al. Histone deacetylase 1 (HDAC1), but not HDAC2, controls embryonic stem cell differentiation. Proc Natl Acad Sci U S A. 2010 May 4;107(18):8242-7.

[5]. Lo Cascio C, et al. Nonredundant, isoform-specific roles of HDAC1 in glioma stem cells. JCI Insight. 2021 Sep 8;6(17):e149232.

[6]. Lee HY, et al. A novel HDAC1/2 inhibitor suppresses colorectal cancer through apoptosis induction and cell cycle regulation. Chem Biol Interact. 2022 Jan 25;352:109778.

Productos relacionados con HDAC1 (294)
Antibodies (1)

Productos relacionados con HDAC1 (294):

By Type:	Pan (177) Selective (60)
By Effects:	Inhibitors (281) Activator (1) Degraders (5) Substrate (1)

Cat. No.	Nombre del producto	Efecto	Pureza

HY-175513

ZWZH-21	Inhibitor
ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC₅₀ values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC₅₀ values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer.

HY-179654

ST13	Inhibitor
ST13, an ortho-hydroxyanilide, is a selective, slow- and tight-binding HDAC1 and HDAC2 inhibitor with IC₅₀s of 23 nM and 49 nM, respectively. ST13 shows a weak inhibition of HDAC3 (IC₅₀ = 4.30 μM) and HDAC6 (IC₅₀ > 10 μM). The induced fit mechanism of ST13 proceeds through a two-step process: first, the enzyme and inhibitor rapidly form a collision complex (EI), which then slowly transforms into the stable complex EI. ST13 induces apoptosis* in cancer cells. ST13 can be used for the study of melanoma and triple-negative breast.

HY-168962

HDAC-IN-88	Inhibitor
HDAC-IN-88 (Compound HJ-9) is the inhibitor for HDAC that inhibits HDAC6, HDAC1, HDAC2, HDAC8 and HDAC3 with IC₅₀s of 0.226, 1.103, 2.308, 3.255 and 3.864 μM, respectively. HDAC-IN-88 inhibits the proliferation of cancer cell HepG2, HCT116 and MV4-11 with IC₅₀ of 5.47, 9.78 and 0.38 μM, inhibits the migration of HCT116, arrests the cell cycle at G0/G1 phase, and induces apoptosis and autophagy in MV4-11. HDAC-IN-88 reduces ROS level and mitochondrial membrane potential. HDAC-IN-88 exhibits antimalarial activity that inhibits P. falciparum 3D7 with EC₅₀ of 165 nM. HDAC-IN-88 also exhibits anti-angiogenic activity.

HY-150595

HDAC6-IN-10	Inhibitor
HDAC6-IN-10 is a highly selective HDAC6 inhibitor with the IC₅₀ of 0.73 nM. HDAC6-IN-10 has 144~10941-fold selectivity over other HDAC isoforms. HDAC6-IN-10 shows anti-proliferative activities against multiple myeloma cells.

HY-181843

HDAC-IN-99	Inhibitor
HDAC-IN-99 is a histone deacetylase (HDAC) inhibitor with an IC₅₀ of 37.73 nM, and it exhibits potent inhibitory activity against HDAC1 (IC₅₀ = 48.09 nM), HDAC2 (IC₅₀ = 300.28 nM) and HDAC6 (IC₅₀ = 9.16 nM). HDAC-IN-99 exerts broad-spectrum antiproliferative activity in various cancer cell lines. HDAC-IN-99 induces S-phase cell cycle arrest and apoptosis in colon cancer cells, increases the acetylation levels of histone H3, histone H4 and α-tubulin, and upregulates the expression of p21 as well as the cleavage of caspase-3. HDAC-IN-99 displays antitumor activity in colon cancer xenograft models. HDAC-IN-99 can be used for the research of colon cancer.

HY-146539

HDAC-IN-35	Inhibitor
HDAC-IN-35 (Compound 14) is a potent, selective HDAC and VEGFR-2 inhibitor, with IC₅₀ values of 0.166 and 13.2 µM for HDAC6 and VEGFR-2, respectively.

HY-147991

PDE5/HDAC-IN-1	Inhibitor
PDE5/HDAC-IN-1 (Compound 26) is a potent phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC₅₀ values of 46.3 nM and 14.5 nM, respectively. PDE5/HDAC-IN-1 induces cell apoptosis and shows anticancer activities.

HY-172133

HDAC3-IN-6	Inhibitor
HDAC3-IN-6 (Compound SC26) is a selective HDAC3 inhibitor with an IC₅₀ of 53 nM. HDAC3-IN-6 dose-dependently induces the expression of PD-L1. HDAC3-IN-6 induces more pronounced Apoptosis and production of ROS. HDAC3-IN-6 exhibits high antitumor efficacy against colorectal cancer.

HY-181577

HDAC6-IN-73	Inhibitor
HDAC6-IN-73 is a highly potent and selective HDAC6 inhibitor with an IC₅₀ of 0.007 μM ± 0.001, ~1771-fold selectivity over HDAC1, ~131-fold selectivity over HDAC8, and antiproliferative activity in hematological cancer cell lines.HDAC6-IN-73 can be used for the research of hematological malignancies.

HY-173520

EGFR/HDAC-IN-1	Inhibitor
EGFR/HDAC-IN-1 (Compound 22c2) is a potent dual inhibitor of epidermal growth factor receptor (EGFR) and histone deacetylase (HDAC) with IC₅₀ values of 4.81 nM, 119.4 nM and 354.8 nM for EGFR, HDAC1 and HDAC3, respectively. EGFR/HDAC-IN-1 blocks the EGFR signaling pathway and affects the histone acetylation status, thereby inhibiting tumor cell proliferation. EGFR/HDAC-IN-1 is promising for research of non-small cell lung cancer (NSCLC).

HY-146351

HDAC-IN-38	Inhibitor
HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5).

HY-180811

ALK/HDAC-IN-2	Inhibitor
ALK/HDAC-IN-2 (Compound 19b) is an ALK/HDAC inhibitor with IC₅₀ values for ALK WT and total HDACs of 8 nM and 1.18 μM, respectively. ALK/HDAC-IN-2 exhibits inhibitory activity against ALK mutants G1202R, F1174L, and L1196M, with IC₅₀ values of 2.74, 9.23, and 34.28 nM, respectively. ALK/HDAC-IN-2 shows potent and selective inhibition against HDAC1 (IC₅₀ = 0.24 μM), while its inhibitory activity against HDAC7, HDAC6, and HDAC11 is weak (IC₅₀ > 10 μM). ALK/HDAC-IN-2 has broad-spectrum anti-proliferative activity against various cancer cells, inducing cell cycle arrest and apoptosis. ALK/HDAC-IN-2 can be used for the study of neuroblastoma.

HY-P11678

HDAC-IN-100	Inhibitor
HDAC-IN-100 is a histone deacetylase inhibitor with an IC₅₀ of 0.038 μM against HDAC1, 0.283 μM against HDAC2, and 0.586 μM against HDAC3. HDAC-IN-100 acts as a chemosensitizer and apoptosis inducer, activates caspase 3/7, and reverses Cisplatin (HY-17394) resistance. HDAC-IN-100 exerts antiproliferative effects in ovarian cancer cells and squamous cancer cells. HDAC-IN-100 is applicable for research related to ovarian cancer, squamous cell carcinoma, and Cisplatin (HY-17394)-resistant squamous cell carcinoma.

HY-176904

JPS004	Degrader
JPS004 is a HDAC1-3 PROTAC degrader. JPS004 can induce degradation of HDAC1-3 and induce histone acetylation. JPS004 can induce cancer cells apoptosis. JPS004 can be used for the research of cancer. (Structure Note: Pink: HDAC1-3 ligand (HY-50934); Blue: VHL ligand (HY-125845); HDAC1-3 ligand-Linker: (HY-176905))

HY-147966

HDAC-IN-43	Inhibitor
HDAC-IN-43 is a potent HDAC 1/3/6 inhibitor with IC₅₀ values of 82, 45, and 24 nM, respectively. HDAC-IN-43 is a weak PI3K/mTOR inhibitors with IC₅₀ values of 3.6 and 3.7 μM, respectively. HDAC-IN-43 shows broad anti-proliferative activity .

HY-152226

MC2590	Inhibitor	98.71%
MC2590 is a potent pyridine-containing histone deacetylase (HDAC) inhibitor. MC2590 is a inhibitor of HDAC1-3, -6, -8, and -10 (class I/IIb-selective inhibitor) with IC₅₀s of 0.015 μM-0.156 μM. MC2590 also inhibits HDAC isoforms HDAC4, HDAC5, HDAC7, HDAC9, HDAC11 with IC₅₀s of 1.35 μM-3.98 μM. MC2625 induces G2/M cell cycle arrest and modulates pro- and anti-apoptotic microRNAs towards apoptosis induction.

HY-179019

HDAC-IN-94	Inhibitor
HDAC-IN-94 is a potent, selective HDAC6 inhibitor (IC₅₀ = 4.5 nM). HDAC-IN-94 shows >1000-fold selectivity over HDAC8 and shows minimal activity against other isoforms (HDAC1-3/10). HDAC-IN-94 induces α-tubulin hyperacetylation, apoptosis, and G2/M cell cycle arrest, exhibiting potent anti-tumor efficacy with low cytotoxicity. HDAC-IN-94 can be used for neuroblastoma and glioblastoma research.

HY-175988

DNMT/HDAC-IN-2	Inhibitor
DNMT/HDAC-IN-2 (Compound Y7) is a DNMT and HDAC inhibitor with IC₅₀ values for DNMT1, HDAC1, and HDAC6 of 365, 0.2, and 8.91 nM respectively. DNMT/HDAC-IN-2 inhibits the proliferation of breast cancer cells. DNMT/HDAC-IN-2 significantly reduces tumor growth in xenografts and transgenic breast cancer mouse models. DNMT/HDAC-IN-2 can be used for the study of breast cancer.

HY-178021

HDAC1-IN-11	Inhibitor
HDAC1-IN-11 (Compound 6) is a HDAC1 inhibitor with an IC₅₀ of 106.6  nM. HDAC1-IN-11 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC1-IN-11 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. HDAC1-IN-11 can be used for chemotherapy of cancers like NSCLC research.

HY-146276

CDK/HDAC-IN-2	Inhibitor
CDK/HDAC-IN-2 is a potent HDAC/CDK dual inhibitor with IC₅₀ of 6.4, 0.25, 45, >1000, 8.63, 0.30, >1000 nM for HDAC1, HDAC2, HDAC3, HDAC6,8, CDK1, CDK2, CDK4,6,7, respectively. CDK/HDAC-IN-2 shows excellent antiproliferative activities. CDK/HDAC-IN-2 induces apoptosis and cell cycle arrest at G2/M phase. CDK/HDAC-IN-2 shows potent antitumor efficacy.

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HDAC1

Productos relacionados con HDAC1 (294)

Antibodies (1)

Productos relacionados con HDAC1 (294):