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.

HDAC1 Verwandte Produkte (294)
Antibodies (1)

HDAC1 Verwandte Produkte (294):

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

Art. -Nr.	Produktname	Wirkung	Reinheit

HY-175030

TNI-97	Inhibitor
TNI-97 is a selective and orally active HDAC6 inhibitor, with an IC₅₀ of 0.2 nM. TNI-97 potently inhibited TNBC cell MDA-MB-453 growth and clonogenicity. TNI-97 induces PANoptosis including apoptosis, necroptosis and pyroptosis in MDA-MB-453 cells. TNI-97 shows antitumor activity in the mice carrying the MDA-MB-453 xenograft or carrying murine-derived TNBC cell allografts. TNI-97 can be used for the study of triple-negative breast cancer.

HY-162769

HDAC3-IN-5	Inhibitor
HDAC3-IN-5 (9c) is a HDAC3 selective inhibitor, with IC₅₀ values of 4.2 nM, 1629 nM and 298.2 nM for HDAC3, HDAC2, HDAC1, respectively. HDAC3-IN-5 (9c) can effectively induce apoptosisin MV4-11 cells in vitro and reduce the expression of anti-apoptotic proteins, the development of HDAC3 selective inhibitors may serve as a potential lead compound to reverse Venetoclax resistance.

HY-172394

ZSNI-21	Inhibitor
ZSNI-21 is a ADAM17/HDAC2 inhibitor with ADAM17 IC₅₀ 0.939 μM and HDAC2 IC₅₀ 0.844 μM. ZSNI-21 regulates the expression of apoptosis-related proteins (Bax, Bcl-2) and Cyclin D1, and induces apoptosis.. ZSNI-21 can be used for the research of hepatocellular carcinoma, breast cancer, and non-small cell lung cancer.

HY-144332

PHD2/HDACs-IN-1	Inhibitor
PHD2/HDACs-IN-1 is a potent PHD2/HDACs hybrid inhibitor (IC₅₀s of 1.15 μM, 19.75 μM, 26.60 μM and 15.98 μM for PHD2, HDAC1, HDAC2 and HDAC6, respectively). PHD2/HDACs-IN-1 is a low-toxicity renoprotective agent for research of cisplatin-induced acute kidney injury (AKI).

HY-10585B

Valproic acid sodium (2:1)	Inhibitor
Valproic acid (VPA) sodium (2:1) is an orally active 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 sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.

HY-144098

HDAC8-IN-2	Inhibitor
HDAC8-IN-2 (compound 5o) is a potent HDAC8 inhibitor, with IC₅₀ values of 0.27 and 0.32 μM for smHDAC8 (Schistosoma mansoni histone deacetylase 8) and hHDAC8, respectively. HDAC8-IN-2 shows significant killing of the schistosome larvae. HDAC8-IN-2 markedly impairs egg laying of adult worm pairs.

HY-159172

HDAC3-IN-4	Inhibitor
HDAC3-IN-4 is a selective and orally active HDAC3 inhibitor with an IC₅₀ of 89 nM. HDAC3-IN-4 induces the degradation of PD-L1 by regulating cathepsin B (CTSB) in the lysosomes, with a DC₅₀ of 5.7 μM. HDAC3-IN-4 shows better selectivity for HDAC3 over HDAC1, HDAC6, HDAC7, and HDAC8.

HY-147934

HDAC8-IN-3	Inhibitor
HDAC8-IN-3 (compound P19) is a potent HDAC8 inhibitor with IC₅₀ value of 9.3 μM and produces thermal stabilization. HDAC8-IN-3 has cytotoxicity and induces apoptosis in leukemic cell lines.

HY-146159

PI3K/HDAC-IN-2	Inhibitor
PI3K/HDAC-IN-2 is a potent dual PI3K/HDAC inhibitor with IC₅₀s of 226 nM, 279 nM, 467 nM, 29 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, respectively, and IC₅₀s of 1.3 nM, 3.4 nM, 972 nM, 17 nM, 12 nM for HDAC1, HDAC2, HDC4, HDAC6, HDAC8, respectively. PI3K/HDAC-IN-2 exhibits PI3Kδ and class I and IIb HDAC selectivity. PI3K/HDAC-IN-2 has remarkable anticancer effects.

HY-169400

HDACs/EZH2-IN-1	Inhibitor
HDACs/EZH2-IN-1 (Compound 22a) is a HDACs/EZH2 inhibitor (EZH2 Y641N inhibition rate at 50 nM: 98%), with selective inhibition against HDAC1 and HDAC6 (IC₅₀: 0.23 μM and 0.07 μM, respectively). HDACs/EZH2-IN-1 exerts a antiproliferative effect on diffuse large B-cell lymphoma cells harboring an EZH2 mutation and on various acute myeloid leukemia cells. HDACs/EZH2-IN-1 has the ability to induce cell differentiation and Apoptosis.

HY-141701

mTOR/HDAC-IN-1	Inhibitor
mTOR/HDAC-IN-1 (Compound 50) is a selective mTOR and HDAC dual inhibitor with IC₅₀ values of 0.49 and 0.91 nM against mTOR and HDAC1, respectively. mTOR/HDAC-IN-1 can be studied as an anti-cancer agent.

HY-144297

HDAC1-IN-3	Inhibitor
HDAC1-IN-3 is a potent Pf HDAC1 inhibitor. HDAC1-IN-3 shows antimalarial activity in wild-type and multidrug-resistant parasite strains. HDAC1-IN-3 shows a significant in vivo killing effect against all life cycles of parasites.

HY-150774

HDAC6/HSP90-IN-2	Inhibitor
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC₅₀s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer.

HY-179272

Wee1/HDAC-IN-1	Inhibitor
Wee1/HDAC-IN-1 is a dual Wee1/HDAC inhibitor with an IC₅₀ of 1.2 nM for Wee1 and IC₅₀ values of 196 nM for HDAC1, 156 nM for HDAC3, and 55 nM for HDAC6. Wee1/HDAC-IN-1 exhibits strong antiproliferative activity against MV4-11 cells with an IC₅₀ of 0.076 μM. Wee1/HDAC-IN-1 selectively binds to Wee1 and HDACs. Wee1/HDAC-IN-1 interferes with DNA damage repair pathways and induces apoptosis in MV4-11 cells. Wee1/HDAC-IN-1 Wee1/HDAC-IN-1 can be used for the research of acute myeloid leukemia (AML).

HY-119316A

CM-545	Inhibitor
CM-545, the cis-isomer of CM-414 (HY-119316), is a dual inhibitor of PDE5, HDAC1, HDAC2, HDAC3, and HDAC6 with pIC₅₀ values of 7.47, 6.65, 6.14, 6.55, and 6.84, repectively.

HY-173160

HDAC1-IN-10	Inhibitor
HDAC1-IN-10 (Compound 2b) is a potent, selective and orally active HDAC1/2 inhibitor with IC₅₀ values of 6 and 190 nM. HDAC1-IN-10 shows IC₅₀ > 50 μM for HDAC3-8. HDAC1-IN-10 can inhibit tumor growth in HCT-116 colon xenograft nude mice model. HDAC1-IN-10 can be used for research of colon cancer.

HY-163535

J208	Inhibitor
J208 is a dual inhibitor for histone deacetylase (HDAC) and DNA methyltransferase (DNMT). J208 inhibits proliferation of cancer cells, as well as the migration/invasion of triple-negative breast cancer (TNBC) cells. J208 induces apoptosis, arrests the cell cycle at G0/G1 phase. J2008 activates the innate immune signalling pathway in TNBC, by inducing the expression of endogenous retroviruses (ERVs).

HY-161868

DLC-50	Inhibitor
DLC-50 is a dual inhibitor for PARP-1 and HDAC-1 with IC₅₀ of 1.2 nM and 31 nM. DLC-50 inhibits the proliferation of cancer cells MDA-MB-436, MDA-MB-231, and MCF-7 with IC₅₀ of 0.3, 2.7 and 2.41 μM. DLC-50 induces apoptosis in MDA-MB-231, arrests the cell cycle at G2 phase.

HY-172891

CDK9/HDAC1/HDAC3-IN-1	Inhibitor
CDK9/HDAC1/HDAC3-IN-1 is dual-functional inhibitor of CDK9 and HDAC. CDK9/HDAC1/HDAC3-IN-1 inhibits the protein activity of CDK9/HDAC/HDAC3 with IC₅₀s of 0.17  μM, 1.73  μM and 1.11 μM for CDK9, HDAC1, and HDAC3, respectively. CDK9/HDAC1/HDAC3-IN-1 inhibits cancer cells by inducing cell apoptosis and cell cycle arrest in the G2/M phase, as well as tumor growth in a murine TNBC MDA-MB-231 xenograft model. CDK9/HDAC1/HDAC3-IN-1 has a broad-spectrum anti-cancer activity, such as breast cancer, cervical cancer, and liver cancer.

HY-169433

Naph-Se-TMZ	Inhibitor
Naph-Se-TMZ is a PROTAC-like HDAC1 degrader. Naph-Se-TMZ can reduce the total HDAC activity in glioma cells and enhance the inhibitory effect of Temozolomide (HY-17364). Naph-Se-TMZ consists of the target protein ligand (red part) Temozolomide (HY-17364), the DNA-targeting intercalator (blue part) Nitro-Naphthalimide-C2-acylamide (HY-169437) and the molecular linker (black part). At the same time, the active control of the target protein ligand is: Temozolomide-amino hydrochloride (HY-169439), and the DNA targeting intercalator + linker is: NNISC-2 (HY-169438).

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HDAC1

HDAC1 Verwandte Produkte (294)

Antibodies (1)

HDAC1 Verwandte Produkte (294):