Droxinostat
Droxinostat structure
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Common Name | Droxinostat | ||
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| CAS Number | 99873-43-5 | Molecular Weight | 243.68700 | |
| Density | 1.252 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C11H14ClNO3 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
| Symbol |
GHS05, GHS07 |
Signal Word | Danger | |
Use of DroxinostatDroxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.IC50 Value: 16.9 μM(HDAC3); 2.47 μM(HDAC6); 1.46 μM(HDAC8)Target: HDAC3/6/8in vitro: Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). the direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat selective inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively, without inhibiting other HDAC members (IC50 > 20 μM). In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis.in vivo: In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells. |
| Name | 4-(4-Chloro-2-methylphenoxy)-N-hydroxybutanamide |
|---|---|
| Synonym | More Synonyms |
| Description | Droxinostat(NS41080) is a selective inhibitor of HDAC3, HDAC6, and HDAC8 with IC50 of 16.9, 2.47 and 1.46 μM, respectively; > 8-fold selective against HDAC3 and no inhibition to HDAC1, 2, 4, 5, 7, 9, and 10.IC50 Value: 16.9 μM(HDAC3); 2.47 μM(HDAC6); 1.46 μM(HDAC8)Target: HDAC3/6/8in vitro: Droxinostat is originally identified as a sensitizer of PPC-1 cells to FAS and TRAIL by downregulating the expression of c-Fas-associated death domain-like interleukin-1-converting enzyme-like inhibitory protein (c-FLIP). the direct targets of Droxinostat remains enigma until recently. It is revealed that in histone deacetylases (HDAC) isoform 1-10, Droxinostat selective inhibits HDAC3, 6, and 8, with IC50 values of 16.9 μM, 2.47 μM, and 1.46 μM, respectively, without inhibiting other HDAC members (IC50 > 20 μM). In MCF-7 breast cancer cells, Droxinostat (10 μM–100 μM) sensitizes cells to apoptosis by decreasing c-FLIPL and c-FLIPS expression, reducing cell survival, and inducing apoptosis.in vivo: In SCID mice models, Droxinostat (30 μM)-treated PPC-1 cells results in decreased distant tumor formation than untreated cells. |
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| Related Catalog | |
| Target |
HDAC8:1.46 μM (IC50) HDAC6:2.47 μM (IC50) HDAC3:16.9 μM (IC50) |
| References |
| Density | 1.252 g/cm3 |
|---|---|
| Molecular Formula | C11H14ClNO3 |
| Molecular Weight | 243.68700 |
| Exact Mass | 243.06600 |
| PSA | 62.05000 |
| LogP | 3.15310 |
| Appearance of Characters | white to off-white |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: ≥20mg/mL |
| Symbol |
GHS05, GHS07 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H302-H315-H318-H335 |
| Precautionary Statements | P261-P280-P305 + P351 + P338 |
| Hazard Codes | Xn |
| Risk Phrases | 22-37/38-41 |
| Safety Phrases | 26-39 |
| RIDADR | NONH for all modes of transport |
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Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
Bioorg. Med. Chem. 23 , 5151-5, (2015) Two of the histone deacetylases, TbDAC1 and TbDAC3, have been reported to be essential genes in trypanosomes. Therefore, we tested the activity of a panel of human histone deacetylase inhibitors (HDAC... |
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Inhibition of Histone Deacetylases Permits Lipopolysaccharide-Mediated Secretion of Bioactive IL-1β via a Caspase-1-Independent Mechanism.
J. Immunol. 195 , 5421-31, (2015) Histone deacetylase (HDAC) inhibitors (HDACi) are clinically approved anticancer drugs that have important immune-modulatory properties. We report the surprising finding that HDACi promote LPS-induced... |
| S1422_Selleck |
| cc-490 |
| Droxinostat |