8-Hydroxyefavirenz是 Efavirenz 的主要代谢物,通过 JNK 和 BimEL 依赖机制诱导人原代肝细胞的凋亡 (apoptosis)。该化合物适用于癌症研究,特别是在探讨肿瘤细胞死亡机制中具有应用潜力。
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Type | HazMat fee for 500 gram (Estimated) |
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Limited Quantity | USD 15-60 |
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Inaccessible (Haz class 6.1), International | USD 150+ |
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Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | JNK ↓ ↑ | JNK1 ↓ ↑ | JNK2 ↓ ↑ | JNK3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Mulberroside A | ✔ | 99%+ | |||||||||||||||||
Loureirin B | ✔ | Calcium Channel,Potassium Channel | 99%+ | ||||||||||||||||
Ginsenoside Re | ✔ | NF-κB | 98% | ||||||||||||||||
(+)-(3R,8S)-Falcarindiol | ✔ | STAT,ERK | 99%+ | ||||||||||||||||
trans-Zeatin | ✔ | p38 MAPK,ERK | 95+% | ||||||||||||||||
Urolithin B | ✔ | ERK,NF-κB | 95% | ||||||||||||||||
Cucurbitacin IIb | ✔ | NF-κB | 99% | ||||||||||||||||
Astragaloside IV | ✔ | Akt,mTOR,NF-κB | 98% | ||||||||||||||||
NDMC101 | ✔ | 99%+ | |||||||||||||||||
DB07268 |
++++
JNK1, IC50: 9 nM |
99%+ | |||||||||||||||||
SP600125 |
+
MKK4, IC50: 0.4 μM |
+++
JNK1, IC50: 40 nM |
+++
JNK2, IC50: 40 nM |
+++
JNK3, IC50: 90 nM |
98% | ||||||||||||||
JNK-IN-7 |
++++
JNK1, IC50: 1.5 nM |
++++
JNK2, IC50: 2 nM |
++++
JNK3, IC50: 0.7 nM |
99% | |||||||||||||||
JNK-IN-8 |
++++
JNK1, IC50: 4.7 nM |
+++
JNK2, IC50: 18.7 nM |
++++
JNK3, IC50: 1 nM |
99%+ | |||||||||||||||
3,3',5-Triiodo-L-thyronine |
++
JNK1, Kd: 240 nM |
++
JNK2, Kd: 290 nM |
+++
JNK3, Kd: 66 nM |
98% | |||||||||||||||
IQ-1S free acid |
+
JNK1, IC50: 390 nM |
++
JNK2, IC50: 360 nM |
+++
JNK3, IC50: 87 nM |
99% | |||||||||||||||
BI-78D3 |
++
JNK, IC50: 280 nM |
++
JNK, IC50: 280 nM |
++
JNK, IC50: 280 nM |
++
JNK, IC50: 280 nM |
99%+ | ||||||||||||||
Bentamapimod |
+++
JNK1, IC50: 80 nM |
+++
JNK2, IC50: 90 nM |
++
JNK3, IC50: 230 nM |
98% | |||||||||||||||
Resveratrol |
+
JNK1, IC50: 50 μM |
98% | |||||||||||||||||
Indirubin-3′-oxime | ✔ | 99%+ | |||||||||||||||||
SU3327 |
+
JNK, IC50: 0.7 μM |
+
JNK, IC50: 0.7 μM |
+
JNK, IC50: 0.7 μM |
+
JNK, IC50: 0.7 μM |
99%+ | ||||||||||||||
JNK Inhibitor VIII |
++++
JNK1, Ki: 2 nM JNK1, IC50: 45 nM |
++++
JNK2, IC50: 160 nM JNK2, Ki: 4 nM |
+++
JNK3, Ki: 52 nM |
98% | |||||||||||||||
Doramapimod | ✔ | 99%+ | |||||||||||||||||
RPI-1 | ✔ | 99% | |||||||||||||||||
TCS JNK 5a |
++
JNK2, pIC50: 6.5 |
++
JNK3, pIC50: 6.7 |
98% | ||||||||||||||||
SP 600125, negative control |
+
JNK2, IC50: 18 μM |
+
JNK3, IC50: 24 μM |
97% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | 8-Hydroxyefavirenz (8-OH-EFV) is a primary metabolite of Efavirenz. It induces apoptosis in primary human hepatocytes via a JNK- and BimEL-dependent mechanism. This compound is utilized in cancer research [1]. 8-Hydroxyefavirenz as a click chemistry reagent, contains an alkyne group, enabling it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing azide groups. |
体外研究 | 8-Hydroxyefavirenz (8-OH-EFV; 1-10 μM; 3-24 h) in primary human hepatocytes, prompts cell death in a time- and concentration-dependent manner, initiating caspase-3 activity at 6 hours [1]. 8-Hydroxyefavirenz (1-10 μM; 6-24 h) triggers mitochondrial ROS production in primary human hepatocytes [1]. 8-Hydroxyefavirenz at a concentration of 10 μM for 3-24 hours, activates JNK, increasing the ratio of phosphorylated JNK to total JNK by 4.2-fold. It also upregulates the mRNA and protein expression of BimEL [1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.02mL 0.60mL 0.30mL |
15.08mL 3.02mL 1.51mL |
30.15mL 6.03mL 3.02mL |
CAS号 | 205754-33-2 |
分子式 | C14H9ClF3NO3 |
分子量 | 331.674 |
别名 | 8-OH-EFV |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,Store in freezer, under -20°C |
溶解度 | |
动物实验配方 |