[CAS NO. 3026728-28-6] HDAC-IN-51
PRODUCTS SPECIFICATIONS [3026728-28-6]
DESCRIPTION [3026728-28-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 436.51 |
| Molecular Formula | C27H24N4O2 |
| SMILES | NC1=CC=CC=C1NC(C2=NC=C(C=C2)NC(C(C3=CC=CC=C3)CC4=CC=CC=C4)=O)=O |
Summary
HDAC-IN-51 is a potent histone deacetylase (HDAC) inhibitor with IC 50 values of 0.32, 0.353, 0.431, 0.515, and 85.4 μM for HDAC10 , HDAC1 , HDAC2 , HDAC3 and HDAC11 , respectively. HDAC-IN-51 induces cell cycle arrest and apoptosis , modulating cell cycle-/apoptosis-related miRNAs expression. HDAC-IN-51 can be used in research of cancer [1] .
IC50 & Target
|
HDAC10 0.32 μM (IC 50 ) |
HDAC1 0.353 μM (IC 50 ) |
HDAC2 0.431 μM (IC 50 ) |
HDAC3 0.515 μM (IC 50 ) |
HDAC11 85.4 μM (IC 50 ) |
In Vitro
HDAC-IN-51 (compound 8d; 1 nM-10 μM; 48 h) has antiproliferative activity with IC
50
values of 0.54, 0.56, and 1.35 μM for K562, HCT116, and A549 cells, respectively
[1]
.
HDAC-IN-51 (1 and 5 μM; 24 and 48 h; U937 leukaemia cells) arrests cell cycle at the G1 phase
[1]
.
HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) induces apoptosis and down-regulates miRNAs with antiapoptotic activity (miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p)
[1]
.
HDAC-IN-51 (1 and 5 μM; 48 h; U937 cells) increases mRNA expression of p21, BAX and BAK, down-regulates cyclin D1 and BCL-2
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | K562, HCT116, and A549 cells |
| Concentration: | 1 nM-10 μM |
| Incubation Time: | 48 hours |
| Result: | Inhibited cell growth in cancer cells. |
Cell Cycle Analysis [1]
| Cell Line: | U937 leukaemia cells |
| Concentration: | 1 and 5 μM |
| Incubation Time: | 24 and 48 hours |
| Result: | Blocked the cell cycle at the G1 phase in U937 leukaemia cells. |
Western Blot Analysis [1]
| Cell Line: | U937 cells |
| Concentration: | 1 and 5 μM |
| Incubation Time: | 48 hours |
| Result: | Down-regulates miRNAs with antiapoptotic activity including miR-17-5p, miR-18-5p, miR-19b-3p, miR-20a-5p,miR-21-5p. |
Western Blot Analysis [1]
| Cell Line: | U937 cells |
| Concentration: | 1 and 5 μM |
| Incubation Time: | 48 hours |
| Result: | Increased mRNA expression of p21, BAX and BAK and down-regulated cyclin D1 and BCL-2 in a dose-dependent manner. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.