Fig. 1 · Structure
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Gintemetostat
NSD2/MMSET Inhibitor
Gintemetostat is a highly specific inhibitor of the NSD2/MMSET histone methyltransferase, exhibiting human NSD2 IC50 values between 0.460-2.17 nM and a NSD2 SET domain IC50 of 2.32 nM. This compound effectively reduces levels of H3K36me2, impairs adhesion and colony formation in multiple myeloma cells, enhances cytotoxicity, and boosts T-cell activation. Gintemetostat also sensitizes resistant multiple myeloma cells to other therapeutic agents, making it a valuable tool for research in multiple myeloma and relapsed or refractory cases.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Inhibitor |
| CAS Number | 2604513-16-6 |
| Applications | NSD2/MMSET Inhibitor |
| Formula | C25H26F4N8O2 |
| Molecular Weight | 546.52 |
| Synonyms | KTX-1001 |
| SMILES | FC(C=C(C(F)=C1)OC)=C1C2=NC=C(N3C[C@](N)(CCC3)[C@H](O)C(F)F)C(CN4C5=NC=NC(N)=C5N=C4)=C2 |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.