Name | SKLB-23bb |
Synonyms | SKLB-23bb HDAC6-IN-1 Butanamide, N-hydroxy-4-[2-methoxy-5-[methyl(2-methyl-4-quinazolinyl)amino]phenoxy]- |
CAS | 1815580-06-3 |
Molecular Formula | C21H24N4O4 |
Molar Mass | 396.44 |
Density | 1.271±0.06 g/cm3(Predicted) |
Solubility | Soluble in DMSO |
pKa | 9.32±0.20(Predicted) |
Storage Condition | -20℃ |
Use | SKLB-23bb is a potent selective HDAC6 inhibitor with an IC50 of 17 nM, 25-fold and 200-fold higher selectivity than inhibition of HDAC1 (IC50=422 nM) and HDAC8 (IC50=3398 nM), respectively. |
In vitro study | In a range of solid and hematological tumor cell lines, SKLB-23bb has toxic effects in the low sub-molar range. In contrast to the selective HDAC6 inhibition that has been reported, SKLB-23bb is more effective against solid tumors. SKLB-23bb can selectively inhibit intracellular HDAC6, but its antitumor activity is independent of hdac6. SKLB-23bb can bind to the colchicine site of β-tubulin and is an inhibitor of microtubule polymerization. It can arrest the cell cycle of tumor cells in the G2-M phase and cause apoptosis. |
In vivo study | In solid tumor models, oral administration of SKLB-23bb can effectively inhibit tumor growth. SKLB-23bb has good pharmacokinetic properties and is orally active. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.522 ml | 12.612 ml | 25.224 ml |
5 mM | 0.504 ml | 2.522 ml | 5.045 ml |
10 mM | 0.252 ml | 1.261 ml | 2.522 ml |
5 mM | 0.05 ml | 0.252 ml | 0.504 ml |
Use | SKLB-23bb is a selective HDAC6 inhibitor with oral bioavailability, the IC50 is less than 100 nM in most cell lines tested; It can be used to disrupt microtubule activity. |
Target | Value |
HDAC6 (Cell-based assay) | <100 nM |