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HDAC-IN-57

🥰Excellent
Catalog No. T77334Cas No. 2716217-79-5

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.

HDAC-IN-57

HDAC-IN-57

🥰Excellent
Purity: 98.38%
Catalog No. T77334Cas No. 2716217-79-5
HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.
Pack SizePriceAvailabilityQuantity
1 mg$195In Stock
5 mg$430In Stock
10 mg$636In Stock
25 mg$987In Stock
50 mg$1,360In Stock
100 mg$1,830In Stock
500 mg$3,680In Stock
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Purity:98.38%
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Product Introduction

Bioactivity
Description
HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.
Targets&IC50
HDAC8:107 nM, HDAC6:2.4 nM, HDAC2:4.71 nM, HDAC1:2.07 nM
In vitro
HDAC-IN-57 (Compound 5e) (1.0 μM, 2.5 μM, 5.0 μM; 48 h) effectively suppresses the migration and invasion of solid tumor cell lines, namely MGC-803, A549, and HCT-116. Furthermore, HDAC-IN-57 demonstrates significant growth inhibition in these solid tumor cell lines, exhibiting IC50 values of 0.45 μM, 1.48 μM, and 0.57 μM, respectively. Additionally, HDAC-IN-57 elicits apoptosis in MGC-803 and HCT-116 cells in a dose-dependent manner. It also exerts inhibitory effects on LSD1 and HDACs within the MGC-803 and HCT-116 cell lines. Moreover, HDAC-IN-57 induces cell cycle arrest in the G2/M phase for both MGC-803 and HCT-116 cells.[1]
HDAC-IN-57 has high metabolic stability in vitro. Retains 86.1% and 87.4% of the parent compound after 1 hour of incubation in human liver (HLM) and rat liver microsomes (RLM), respectively, with a T1/2 of over 120 minutes.[1]
In vivo
HDAC-IN-57 (Compound 5e) (1 mg/kg, i.v.; 10 mg/kg, p.o.) demonstrated T1/2 of 0.37 hours (IV) and 2.75 hours (OR), with an oral bioavailability (F%) of 10.6%.[1]
HDAC-IN-57 (25 or 50 mg/kg gavage; once daily for 21 days) achieved dose-dependent tumor growth inhibition in the NOD-SCID mouse MGC-803 xenograft model.[1]
Chemical Properties
Molecular Weight377.39
FormulaC21H19N3O4
Cas No.2716217-79-5
SmilesC(NCC1=CC=C(C(NO)=O)C=C1)(=O)C=2C=C(N=CC2)C3=CC=C(OC)C=C3
Relative Density.1.282 g/cm3 at 20℃ (Predicted)
Storage & Solubility Information
StorageShipping with blue ice.
Solubility Information
DMSO: 45 mg/mL (119.24 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.6498 mL13.2489 mL26.4978 mL132.4889 mL
5 mM0.5300 mL2.6498 mL5.2996 mL26.4978 mL
10 mM0.2650 mL1.3249 mL2.6498 mL13.2489 mL
20 mM0.1325 mL0.6624 mL1.3249 mL6.6244 mL
50 mM0.0530 mL0.2650 mL0.5300 mL2.6498 mL
100 mM0.0265 mL0.1325 mL0.2650 mL1.3249 mL

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