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HDAC-IN-53

Catalog No. T74783 CAS 2921948-27-6

HDAC-IN-53 is an orally active, selective inhibitor of HDAC1-3, demonstrating IC50 values of 47 nM, 125 nM, and 450 nM, respectively. It exhibits no inhibitory effects on class II HDACs (HDAC4, 5, 6, 7, 9; IC50 <10 μM). The compound induces caspase-dependent apoptosis and significantly hampers the growth of human tumor xenografts in nude mice, as well as murine tumor growth in immune-competent mice with MC38 colon cancer [1].

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HDAC-IN-53, CAS 2921948-27-6

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,520.00
50 mg	8-10 weeks	$ 1,980.00
100 mg	8-10 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.

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Description	HDAC-IN-53 is an orally active, selective inhibitor of HDAC1-3, demonstrating IC50 values of 47 nM, 125 nM, and 450 nM, respectively. It exhibits no inhibitory effects on class II HDACs (HDAC4, 5, 6, 7, 9; IC50 >10 μM). The compound induces caspase-dependent apoptosis and significantly hampers the growth of human tumor xenografts in nude mice, as well as murine tumor growth in immune-competent mice with MC38 colon cancer [1].
Targets&IC50	HDAC1:47 nM, HDAC2:125 nM, HDAC3:450 nM, HDAC4:>10 μM, HDAC5:>10 μM, HDAC6:>10 μM, HDAC7:>10 μM, HDAC8:>10 μM, HDAC9:>10 μM
In vitro	HDAC-IN-53 (Compound 19h) exhibits robust antiproliferative activity against a panel of cancer cell lines, such as MC38 (IC50 = 0.66 μM) and HCT116 cells (IC50 = 0.56 μM) [1]. At concentrations ranging from 0.1 to 1 μM over 24 hours, HDAC-IN-53 induces G0/G1 cell cycle arrest in MC38 cells and G2/M cell cycle arrest in HCT116 cells [1]. Additionally, the same treatment with HDAC-IN-53 dose-dependently upregulates the expression of cleaved caspase-3 and cleaved PARP [1].
In vivo	HDAC-IN-53, administered orally at doses of 60 or 120 mg/kg once daily for 15 days, exhibited antitumor activity through both direct inhibition of tumor growth and indirect immune cell-mediated antitumor effects[1]. The pharmacokinetic parameters of HDAC-IN-53 in mice are reported as follows[1]: after intravenous (IV) administration at 5 mg/kg, the time to maximum concentration (Tmax) is 0.42 hours, with a maximum concentration (Cmax) of 8129 ng/mL. The area under the curve (AUC0-t) is 5864 ng/mL∗h, and the half-life (t1/2) is 0.85 hours. In contrast, after oral administration (PO) at 20 mg/kg, Tmax is 0.42 hours, Cmax is 9558 ng/mL, AUC0-t is 15278 ng/mL∗h, t1/2 is 2.49 hours, and the bioavailability (F%) is 65.1%.

Molecular Weight	461.9
Formula	C23H20ClN7O2
CAS No.	2921948-27-6

Storage

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

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Keywords

HDAC-IN-53 2921948-27-6 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC inhibitor inhibit

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