Molecular Formula | C21H21NO.ClH |
Molar Mass | 339.864 |
Solubility | DMSO: ≥2mg/mL (warmed) |
Appearance | powder |
Color | faint yellow to dark yellow |
Storage Condition | Store at +4°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
In vitro study | NSC 632839 inhibited purified USP2-and usp7-regulated cleavage by Ub-PLA2. Within the experimental concentration range (1.2-150 μm), the receptor enzyme PLA2 was not inhibited, indicating that NSC 632839 selectively inhibits isopeptidase. NSC 632839 acts on E1A and E1A/C9DN cells and maintains caspase-3/caspase-9 activity in the absence of functional caspase-7. NSC 632839 induced apoptosis in E1A and E1A/C9DN cells with an IC50 of 15.65 μm and 16.23 μm, respectively. NSC-632839 (10 μm) acts on E1A cells expressing HA-tagged ubiquitin to promote the accumulation of polymeric ubiquitin. NSC-632839 (10 μm) significantly increased Noxa and Mcl-1 levels in E1A cells in a time course assay. Compared to Etoposide, NSC-632839(10 μm) acts on cells with intact mitochondrial outer membrane, promoting a higher proportion of mitochondrial division. |
Risk Codes | R36 - Irritating to the eyes R51/53 - Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9 / PGIII |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.942 ml | 14.712 ml | 29.424 ml |
5 mM | 0.588 ml | 2.942 ml | 5.885 ml |
10 mM | 0.294 ml | 1.471 ml | 2.942 ml |
5 mM | 0.059 ml | 0.294 ml | 0.588 ml |
biological activity | NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor, acting on USP2, USP7, and SENP2, EC50 are 45 μM, 37 μM and 9.8 μM respectively. |
target | TargetValue SENP2 (Cell-free say) 9.8 μM(EC50) USP7 (Cell-free say) 37 μM(EC50) USP2 (Cell-free say) 45 μM(EC50) |
Target | Value |
SENP2 (Cell-free assay) | 9.8 μM(EC50) |
USP7 (Cell-free assay) | 37 μM(EC50) |
USP2 (Cell-free assay) | 45 μM(EC50) |
In vitro study | NSC 632839 inhibits purified USP2-and USP7-regulated Ub-PLA2 cleavage. The receptor enzyme PLA2 was not inhibited in the experimental concentration range (1.2-150 μM), indicating that NSC 632839 selectively inhibit isopeptidase. NSC 632839 acts on E1A and E1A/C9DN cells and can maintain caspase-3/caspase-7 activity in the absence of functional caspase-9. NSC 632839 acts on E1A and E1A/C9DN cells to induce apoptosis with IC50 of 15.65 μM and 16.23 μM respectively. NSC-632839 (10 μM) acts on E1A cells expressing HA tag ubiquitin to promote the accumulation of polyubiquitin. NSC-632839 (10 μM) acts on E1A cells, significantly increasing Noxa and Mcl-1 levels in a time course analysis. Compared with Etoposide, NSC-632839(10 μM) acts on cells with intact mitochondrial outer membrane, promoting a higher proportion of mitochondrial division. |