N-Hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide
PCI-34051
CAS: 950762-95-5
Molecular Formula: C17H16N2O3
N-Hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide - Names and Identifiers
N-Hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide - Physico-chemical Properties
| Molecular Formula | C17H16N2O3 |
| Molar Mass | 296.32 |
| Density | 1.25 |
| pKa | 9.16±0.30(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | PCI-34051 effective on HDAC8,K I is 10 nM. Compared to other Type I HDACs, including HDAC1, PCI-34051 was more selective for hdac8. The selectivity was 200-fold higher for HDAC1 and HDAC6 and 1000-fold higher for HDAC2, HDAC3 and hdac10. PCI-34051 inhibition of ovarian tumor cell line OVCAR-3,GI50 6 μm, Mortality Rate cells 15%. At PCI-34051 concentrations below 25 μm, no significant tubulin and no histone acetylation was observed in sensitive cell lines treated at 24 hours, but not at earlier time points. PCI-34051 acts on T-cell malignant-derived cell lines, inducing selective cytotoxic effects. PCI-34051 induced caspase-dependent apoptosis. caspase-3 activity was measured at different time points after treatment with 5 μm PCI-34051, and increased activity levels were observed from 12 to 24 to 48 hours, another marker of apoptosis, consistent with higher levels of caspase activity. PCI-34051 does not stimulate Bid Division, a characteristic effect of the extrinsic apoptotic pathway. P116 and J.RT3-T.5 were PCI-34051 sensitive, and PLCγ1 deficient J.gamma1 lines significantly reduced the extent of PCI-34051 induced apoptosis. In addition, stable calcium levels also strongly affect PCI-34051-induced apoptosis. PCI-34051 induction of cytochrome c release from mitochondria. |
N-Hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide - Risk and Safety
| Hazard Symbols | Xn - Harmful |
| Risk Codes | R22 - Harmful if swallowed R36 - Irritating to the eyes |
| Safety Description | 26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
N-Hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.375 ml | 16.874 ml | 33.747 ml |
| 5 mM | 0.675 ml | 3.375 ml | 6.749 ml |
| 10 mM | 0.337 ml | 1.687 ml | 3.375 ml |
| 5 mM | 0.067 ml | 0.337 ml | 0.675 ml |
Last Update：2024-01-02 23:10:35
N-Hydroxy-1-[(4-methoxyphenyl)methyl]-1H-indole-6-carboxamide - Reference Information
| biological activity | PCI-34051 is an effective and specific HDAC8 inhibitor with IC50 of 10 nM in cell-free test. More than 200 times higher selectivity than HDAC1 and 6, and 1000 times higher selectivity than HDAC2, 3, and 10. PCI-34051 induces caspase-dependent apoptosis. |
| target | TargetValue HDAC8 (Cell-free say) 10 nM |
| Target | Value |
| HDAC8 (Cell-free assay) | 10 nM |
| in vitro study | PCI-34051 effectively act on HDAC8,K I is 10 nM. Compared with other type I HDACs including HDAC1, PCI-34051 is more selective to act on HDAC8. The selectivity is 200 times higher than that of HDAC1 and HDAC6, and 1000 times higher than that of HDAC2, HDAC3 and HDAC10. PCI-34051 inhibited ovarian tumor cell line OVCAR-3,GI50 was 6 μM, and cell mortality was 15%. When the PCI-34051 concentration is lower than 25 μM, no significant tubulin or histone acetylation is observed in the sensitive cell line at 24 hours instead of earlier time points. PCI-34051 acts on T cell malignant tumor-derived cell lines to induce selective cytotoxic effects. PCI-34051 induces caspase-dependent apoptosis. After treatment with 5 μM PCI-34051, caspase-3 activity was measured at different time points. An increase in activity level was observed at 12 to 24 to 48 hours, another sign of apoptosis, consistent with higher levels of caspase activity. PCI-34051 does not stimulate Bid division, Bid division is a characteristic influence of external apoptotic pathway. P116 and J.RT3-T.5 are sensitive to PCI-34051. J.gamma1 line with PLCγ1 deficiency significantly reduces the degree of apoptosis induced by PCI-34051. In addition, stable calcium levels also strongly affect PCI-34051-induced apoptosis. PCI-34051 induces the release of cytochrome c from mitochondria. |
Last Update：2024-04-09 21:54:55
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Spot supply
Product Name: PCI-34051 Visit Supplier Webpage Request for quotationCAS: 950762-95-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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