Molecular Formula | C24H19N3O6 |
Molar Mass | 445.42 |
Density | 1.38±0.1 g/cm3(Predicted) |
Melting Point | 224-226℃ |
Boling Point | 662.6±65.0 °C(Predicted) |
Solubility | DMSO: >25mg/mL |
Appearance | powder |
Color | red to brown |
pKa | 4.20±0.10(Predicted) |
Storage Condition | 2-8°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 2 months. |
In vitro study | C646 is a histone acetyltransferase inhibitor that inhibits p300 with a Ki of 400 nM and acts selectively on other acetyltransferases. 10 M C646 inhibited 86% of p300 in vitro. C646 is a traditional, reversible p300 inhibitor. C646(25 μm) acts on cells to reduce the level of histone H3 and H4 acetylation and abrogates TSA-induced acetylation. C646(20 μm) acts on androgen-sensitive castrated prostate cancer cell lines, inducing apoptosis by interfering with the AR and NF-kB pathways. C646 acts on mouse cells, inhibits all H3K4me3 dynamic acetylation, and locally spans the start site of the promoter and induced genes, thereby interfering with RNA polymerase II interactions and activation of these genes. C646 is a histone acetyltransferase inhibitor that inhibits p300,K I at 400 nM and acts selectively on other acetyltransferases. 10 M C646 inhibited 86% of p300 in vitro. C646 is a traditional, reversible p300 inhibitor. C646(25 μm) acts on cells to reduce the level of histone H3 and H4 acetylation and abrogates TSA-induced acetylation. C646(20 μm) acts on androgen-sensitive castrated prostate cancer cell lines, inducing apoptosis by interfering with the AR and NF-kB pathways. C646 acts on mouse cells, inhibits all H3K4me3 dynamic acetylation, and locally spans the start site of the promoter and induced genes, thereby interfering with RNA polymerase II interactions and activation of these genes. |
In vivo study | After weak extinction training, C646 was injected into ILPFC immediately to enhance the integration of fear extinction memory. C646 treated the spinal cord, attenuating mechanical pain and thermal hyperalgesia, with concomitant inhibition of COX-2 expression. after weak extinction training, C646 was injected into ILPFC immediately to enhance the integration of fear extinction memory. C646 treated the spinal cord, attenuating mechanical pain and thermal hyperalgesia, with concomitant inhibition of COX-2 expression. |
Hazard Symbols | N - Dangerous for the environment |
Risk Codes | 50 - Very Toxic to aquatic organisms |
Safety Description | 61 - 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 | 2.245 ml | 11.225 ml | 22.451 ml |
5 mM | 0.449 ml | 2.245 ml | 4.49 ml |
10 mM | 0.225 ml | 1.123 ml | 2.245 ml |
5 mM | 0.045 ml | 0.225 ml | 0.449 ml |
biological activity | C646 is a histone acetyltransferase inhibitor that inhibits p300, ki is 400 nM, which is more selective than other acetyltransferases. C646 is a histone acetyl transferase inhibitor that inhibits p300, with a Ki of 400 nM in the cell-free assay, preferentially acting on p300 compared to other acetyltransferases. C646 can induce cell cycle arrest, apoptosis and autophagy. |
in vitro study | C646 is a histone acetyltransferase inhibitor that inhibits p300 with a Ki of 400 nM, selective action on other acetyltransferases. 10 M C646 inhibited 86% of p300 in vitro. C646 is a traditional, reversible p300 inhibitor. C646(25 μm) acts on cells to reduce the level of histone H3 and H4 acetylation and abrogates TSA-induced acetylation. C646(20 μm) acts on androgen-sensitive castrated prostate cancer cell lines, inducing apoptosis by interfering with the AR and NF-kB pathways. C646 acts on mouse cells, inhibits all H3K4me3 dynamic acetylation, and locally spans the start site of the promoter and induced genes, thereby interfering with RNA polymerase II interactions and activation of these genes. C646 is a histone acetyltransferase inhibitor that inhibits p300,K I at 400 nM and acts selectively on other acetyltransferases. 10 M C646 inhibited 86% of p300 in vitro. C646 is a traditional, reversible p300 inhibitor. C646(25 μm) acts on cells to reduce the level of histone H3 and H4 acetylation and abrogates TSA-induced acetylation. C646(20 μm) acts on androgen-sensitive castrated prostate cancer cell lines, inducing apoptosis by interfering with the AR and NF-kB pathways. C646 acts on mouse cells, inhibits all H3K4me3 dynamic acetylation, and locally spans the start site of the promoter and induced genes, thereby interfering with RNA polymerase II interactions and activation of these genes. |
in vivo study | after weak extinction training, C646 was injected into ILPFC immediately to enhance the integration of fear extinction memory. C646 treated the spinal cord, attenuating mechanical pain and thermal hyperalgesia, with concomitant inhibition of COX-2 expression. after weak extinction training, C646 was injected into ILPFC immediately to enhance the integration of fear extinction memory. C646 treated the spinal cord, attenuating mechanical pain and thermal hyperalgesia, with concomitant inhibition of COX-2 expression. |
features | extensible used as a pharmacologic probe in cancer cells. Potential use for prostate and lung cancer. |
Target | TargetValue p300/CBP (Cell-free assay) 400 nM(Ki) |
Target | Value |
p300/CBP (Cell-free assay) | 400 nM(Ki) |