Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 195.00 | |
5 mg | In stock | $ 430.00 | |
10 mg | In stock | $ 636.00 | |
25 mg | In stock | $ 987.00 | |
50 mg | In stock | $ 1,360.00 | |
100 mg | In stock | $ 1,830.00 | |
500 mg | In stock | $ 3,680.00 |
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 | HDAC1:2.07 nM, HDAC2:4.71 nM, HDAC6:2.4 nM, HDAC8:107 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] |
Molecular Weight | 377.39 |
Formula | C21H19N3O4 |
CAS No. | 2716217-79-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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HDAC-IN-57 2716217-79-5 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC HDACIN57 inhibitor inhibit