シリオブレビンA
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- CAS番号.
- 302803-72-1
- 化学名:
- シリオブレビンA
- 别名:
- シリオブレビンA;3-(2,4-ジクロロフェニル)-3-オキソ-2-(4-オキソ-1,2,3,4-テトラヒドロキナゾリン-2-イリデン)プロパンニトリル;1,2-ジヒドロ-2-[1-シアノ-2-オキソ-2-(2,4-ジクロロフェニル)エチリデン]キナゾリン-4(3H)-オン
- 英語名:
- HPI-4,Hedgehog Pathway Inhibitor 4
- 英語别名:
- HPI-4;iobrevin A;HPI-4;HPI 4;Ciliobrevin A;Ciliobrevin A(HPI4);HPI-4 (Ciliobrevin A);Hedgehog Pathway Inhibitor 4;HPI-4,Hedgehog Pathway Inhibitor 4;HPI4,Hedgehog,HPI 4,Ciliobrevin A,inhibit,Inhibitor;2,4-Dichloro-α-(3,4-4-oxo-2(1H)-quinazolinylidene)-β-oxobenzenepropanenitrile
- CBNumber:
- CB72644957
- 化学式:
- C17H9Cl2N3O2
- 分子量:
- 358.18
- MOL File:
- 302803-72-1.mol
- MSDS File:
- SDS
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シリオブレビンA 物理性質
- 沸点 :
- 564.5±50.0 °C(Predicted)
- 比重(密度) :
- 1.471±0.06 g/cm3(Predicted)
- 貯蔵温度 :
- 2-8°C
- 溶解性:
- DMSO：可溶10mg/mL、透明
- 酸解離定数(Pka):
- 6.46±0.20(Predicted)
- 外見 :
- 粉
- 色:
- オフホワイト、オフホワイトからオレンジ
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01TOC4529 |
Ciliobrevin A |
302803-72-1 |
5mg |
￥36000 |
2024-03-01 |
購入 |
|
富士フイルム和光純薬株式会社(wako)
|
W01TOC4529 |
Ciliobrevin A |
302803-72-1 |
25mg |
￥136000 |
2024-03-01 |
購入 |
|
Sigma-Aldrich Japan
|
H4541 |
≥98% (HPLC)
HPI-4 ≥98% (HPLC) |
302803-72-1 |
5mg |
￥26400 |
2024-03-01 |
購入 |
|
Sigma-Aldrich Japan
|
H4541 |
≥98% (HPLC)
HPI-4 ≥98% (HPLC) |
302803-72-1 |
25mg |
￥79800 |
2024-03-01 |
購入 |
シリオブレビンA 化学特性,用途語,生産方法
説明
Ciliobrevin A is a hedgehog pathway inhibitor that blocks sonic hedgehog (Shh)-induced hedgehog pathway activation (IC
50 = 7 μM). It disrupts primary cilia formation and inhibits the dynein-dependent microtubial gliding and ATPase activities of the cytoplasmic ATPases associated with various cellular activities (AAA+) family. Ciliobrevin A also inhibits mammalian target of rapamycin complex 1 (mTORC1) activity in uninfected and human cytomegalovirus (HCMV)-infected cells, suggesting that mTORC1 activation requires dynein-dependent transport for cellular activation.
使用
Ciliobrevin A is a Hedgehog pathway inhibitor; ciliogenesis inhibitor. The Hedgehog (HH) signaling pathway is targeted for anti-cancer therapeutics. Ciliobrevin A inhibited proliferation of cerebellar granula neuron precursor cells, an important model of HH signaling.
Biochem/physiol Actions
HPI-4 is a Hedgehog pathway inhibitor; ciliogenesis inhibitor. The Hedgehog (HH) signaling pathway is targeted for anti-cancer therapeutics. A key signaling molecule in HH pathway, Smoothened (Smo), has been the target of pharmacological intervention, which has resulted in multiple Smo antagonists including Cyclopamine. However, the oncogenic form of Smo is resistant to Cyclopamine, so the identification of inhibitors of downstream effectors, such as the transcription factors Gli1 and Gli2, is important. Four small molecules were identified to inhibit HH downstream of Smo, HPI-1, HPI-2, HPI-3, and HPI-4. HPI-4 blocked HH pathway activation by SAG, decreased Smo ciliary accumulation, decreased HH activity in a consitutively active HH cell line, and decreased Gli1 and Gli2, processing, and stability. HPI-4 inhibited proliferation of cerebellar granula neuron precursor cells, an important model of HH signaling. Cilia in HPI-4-treated cells were either truncated or absent. The mechanism of action of HPI-4 is hypothesized to be directly through perturbation of ciliogenesis, leading to disruption of Gli1/Gli2 activity, which is distinctly different from that of Cyclopamine.
シリオブレビンA 上流と下流の製品情報
原材料
準備製品
シリオブレビンA 生産企業
Global( 78)Suppliers
- 302803-72-1
- HPI-4
- HPI-4,Hedgehog Pathway Inhibitor 4
- Ciliobrevin A
- Ciliobrevin A(HPI4)
- 2,4-Dichloro-a-(3,4-dihydro-4-oxo-2(1H)-quinazolinylidene)-β-oxo-benzenepropanenitrile
- Hedgehog Pathway Inhibitor 4
- 2-(7-Chloro-4-oxo-3,4-dihydro-1H-quinazolin-2-ylidene)-3-(2,4-dichloro-phenyl)-3-oxo-propionitrile
- (Z)-3-(2,4-dichlorophenyl)-3-oxo-2-(4-oxo-3,4-dihydroquinazolin-2(1H)-ylidene)propanenitrile
- 2,4-Dichloro-α-(3,4-4-oxo-2(1H)-quinazolinylidene)-β-oxobenzenepropanenitrile
- HPI-4;HPI 4
- HPI-4 (Ciliobrevin A)
- iobrevin A
- Benzenepropanenitrile, 2,4-dichloro-α-(3,4-dihydro-4-oxo-2(1H)-quinazolinylidene)-β-oxo-
- (E)-3-(2,4-dichlorophenyl)-3-oxo-2-(4-oxo-3,4-dihydroquinazolin-2(1H)-ylidene)propanenitrile
- 3-(2,4-Dichlorophenyl)-3-oxo-2-(4-oxo-3,4-dihydroquinazolin-2(1H)-ylidene)propanenitrile
- HPI4,Hedgehog,HPI 4,Ciliobrevin A,inhibit,Inhibitor
- シリオブレビンA
- 3-(2,4-ジクロロフェニル)-3-オキソ-2-(4-オキソ-1,2,3,4-テトラヒドロキナゾリン-2-イリデン)プロパンニトリル
- 1,2-ジヒドロ-2-[1-シアノ-2-オキソ-2-(2,4-ジクロロフェニル)エチリデン]キナゾリン-4(3H)-オン