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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 | Price | Availability | Quantity |
---|---|---|---|
1 mg | $195 | In Stock | |
5 mg | $430 | In Stock | |
10 mg | $636 | In Stock | |
25 mg | $987 | In Stock | |
50 mg | $1,360 | In Stock | |
100 mg | $1,830 | In Stock | |
500 mg | $3,680 | In Stock |
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] |
Molecular Weight | 377.39 |
Formula | C21H19N3O4 |
Cas No. | 2716217-79-5 |
Smiles | C(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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 45 mg/mL (119.24 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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