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NB512 (compound 39a) is a dual inhibitor targeting both BET and HDAC, exhibiting high affinity for the BRD4 bromodomain and HDAC1/2, with EC50 values ranging from 100 to 400 nM. It demonstrates antiproliferative activity in cancer cell lines PaTu8988T and NMC.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | NB512 (compound 39a) is a dual inhibitor targeting both BET and HDAC, exhibiting high affinity for the BRD4 bromodomain and HDAC1/2, with EC50 values ranging from 100 to 400 nM. It demonstrates antiproliferative activity in cancer cell lines PaTu8988T and NMC. |
| Targets&IC50 | BRD4 BD2:0.25 μM (EC50), HDAC2:0.1 μM (EC50), HDAC1:0.11 μM (EC50), BRD4 BD1:0.36 μM (EC50), HDAC3:13.6 μM (EC50) |
| In vitro | NB512 at a concentration of 1 μM inhibits histone H3 K9/K14 deacetylation and increases the expression of BET target marker HEXIM1 and cell cycle regulatory gene p57 in a dose-dependent manner in PaTu8988T cells. This compound exhibits antiproliferative activity in PaTu8988T and NMC cells, with IC50 values of 3.6 and 0.42 μM, respectively. Additionally, NB512 at 1 μM reduces the expression of oncogenic transcription factors MYC and TP63 in NMC cells. |
| Formula | C26H21N5O2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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