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HDAC1-IN-5

Catalog No. T61433

HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1]

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

HDAC1-IN-5, CAS N/A

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 1,520.00
50 mg	10-14 weeks	$ 1,980.00
100 mg	10-14 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	HDAC1-IN-5, a potent inhibitor of HDAC1 with an IC50 value of 15 nM, also exhibits inhibitory activity towards HDAC6 with an IC50 value of 20 nM. In cancer cells, HDAC1-IN-5 enhances the acetylation of both histone H3 and α-tubulin, leading to the activation of caspase 3 and induction of apoptosis. Additionally, HDAC1-IN-5 binds with DNA, causing chromatin damage. Furthermore, it demonstrated strong inhibitory activity against tumor growth in xenograft mice. [1]
In vitro	HDAC1-IN-5 (compound 4j), across a range of concentrations (0-50 μM; 48 h), demonstrates potent inhibitory effects on several cell lines, including HCT116, HeLa, HepG2, MC38, K562, and HEL, exhibiting IC50 values of 0.47 μM, 0.78 μM, 1.4 μM, 0.43 μM, 0.91 μM, and 0.28 μM, respectively [1]. At lower concentrations (0.16-1.5 μM; 48 h), HDAC1-IN-5 triggers apoptosis in HCT116 cells in a dose-dependent manner, inducing 38.5% apoptosis at 1.5 μM [1]. Additionally, HDAC1-IN-5 (0.17-1.5 μM; 24 h or 48 h) leads to the downregulation of SPT16 and SSRP-1, caspase-3 cleavage, and an increase in Acetyl-Histone H3 and Acetyl-α-tubulin expression in HCT116 and MC38 cells, demonstrating a mechanism involving modulation of both cell proliferation and apoptotic pathways in a dose-dependent fashion [1].
In vivo	HDAC1-IN-5 administered intraperitoneally (IP) at dosages of 50 and 100 mg/kg every two days for 16 days significantly reduced tumor volume and weight in MC38 xenograft mice models composed of C57BL/6 mice aged 6-10 weeks, into which 2×10^6 MC38 cells were subcutaneously injected into the right flank regions. This therapy achieved a tumor growth inhibition (TGI) rate of 66% at the 50 mg/kg dosage.

Molecular Weight	367.46
Formula	C20H21N3O2S

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

HDAC1-IN-5 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.