货号:A116360 同义名: 恩贝酸/恩贝灵 / Emberine;NSC 91874
Embelin, a quinone isolated from the Japanese Ardisia herb, is an inhibitor of X-linked inhibitor of apoptosis (XIAP) with IC50 of 4.1 μM in a cell-free assay.
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | cIAP ↓ ↑ | XIAP ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
LCL161 | ✔ | 99%+ | |||||||||||||||||
AZD5582 |
+++
cIAP2, IC50: 21 nM cIAP1, IC50: 15 nM |
+++
XIAP, IC50: 15 nM |
99%+ | ||||||||||||||||
Birinapant |
++++
cIAP1, Kd: <1 nM |
++
XIAP, Kd: 45 nM |
98+% | ||||||||||||||||
GDC-0152 |
+++
cIAP1-BIR3, Ki: 17 nM cIAP2-BIR3, Ki: 43 nM |
++
XIAP-BIR3, Ki: 28 nM XIAP-BIR2, Ki: 112 nM |
99%+ | ||||||||||||||||
Xevinapant |
++++
cIAP1-BIR3, Ki: 1.9 nM cIAP2-BIR3, Ki: 5.1 nM |
+
XIAP-BIR3, Ki: 66.4 nM |
99%+ | ||||||||||||||||
Embelin |
+
XIAP, IC50: 4.1 μM |
99%+ | |||||||||||||||||
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。 |
靶点 |
|
描述 | Embelin is a potent XIAP inhibitor with IC50 value of 4.1μM (measured by FP-based biochemical binding assay) [1]. Pretreatment with embelin 12h prior to TNFα at concentration ranging in 10-50μM can dose-dependently inhibit TNFα-induced NF-κB activation by inhibiting IκB degradation, as well as inhibted TNFα-induced p65 nuclear translocation due to inhibition of p65 phosphorylation in KBM-5 cells. with no affect on protein level of IAP1, IAP2 and XIAP. Exposure to 50μM embelin for 6-24h could reduce the antiapoptotic proteins survivin, IAP1/2, and suppress Bcl-xL, cFLIP, and TRAF1, suppress the cell proliferation gene expression, including COX-2, cyclin D1 and c-Myc, as well as gene products involved in tumor metastasis, including VEGF, MMP-9 and ICAM-1, which were all TNF-induced NF-κB-dependent[2]. The induction of autophagic and apoptotic cell death by embelin can also be observed in human oral squamous cell carcinoma Ca9-22 cell line[3]. Neonatal injections of 20mg/kg embelin, s.c., could exacerbate hypoxia-ischemia-induced persistent behavioral deficits in female rats on postnatal day 7, but not in male rats[4]. |
作用机制 | Embelin bind to the XIAP-BIR3 domain where caspase-9 and Smac proteins bind. [1] |
Dose | Rat: min = 15 mg/kg, max = 120 mg/kg[5] (p.o.); 5 mg/kg[5] (i.v.); 0.3 mg/kg - 1.2 mg/kg[6] (i.p.) | ||||||||||||||||||||
Administration | p.o., i.v., i.p. | ||||||||||||||||||||
Pharmacokinetics |
|
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02785172 | Psoriasis | Phase 2 | Completed | - | United States, California ... 展开 >> Valeant Site 12 Fullerton, California, United States, 92831 Valeant Site 04 La Mesa, California, United States, 91941 Valeant Site 03 San Diego, California, United States, 92093 Valeant Site 09 San Diego, California, United States, 92093 United States, Florida Valeant Site 05 Lauderdale Lakes, Florida, United States, 33313 Valeant Site 02 Miami, Florida, United States, 33111 United States, Minnesota Valeant Site 07 Fridley, Minnesota, United States, 55421 United States, North Carolina Valeant Site 08 Chapel Hill, North Carolina, United States, 27514 United States, Ohio Valeant Site 06 Columbus, Ohio, United States, 43085 United States, South Carolina Valeant Site 13 Mount Pleasant, South Carolina, United States, 29464 United States, Texas Valeant Site 11 Katy, Texas, United States, 77449 Valeant Site 10 San Antonio, Texas, United States, 78201 Valeant Site 01 Sugar Land, Texas, United States, 77479 United States, Utah Valeant Site 14 Salt Lake City, Utah, United States, 84103 收起 << |
NCT03058744 | Psoriasis | Phase 1 | Completed | - | United States, California ... 展开 >> Valeant Site 12 Anaheim, California, United States, 92801 Valeant Site 05 Encino, California, United States, 91436 Valeant Site 01 San Diego, California, United States, 92093 Valeant Site 07 Santa Rosa, California, United States, 95401 United States, Florida Valeant Site 10 Orange Park, Florida, United States, 32065 Valeant Site 09 Sanford, Florida, United States, 32771 United States, Georgia Valeant Site 08 Atlanta, Georgia, United States, 30301 United States, Indiana Valeant Site 04 Plainfield, Indiana, United States, 46168 United States, New York Valeant Site 06 New York, New York, United States, 10001 United States, Pennsylvania Valeant Site 11 Philadelphia, Pennsylvania, United States, 19019 United States, Texas Valeant Site 03 Austin, Texas, United States, 73301 Valeant Site 02 Katy, Texas, United States, 77449 收起 << |
NCT01567215 | Fetus or Newborn Affected by C... 展开 >>ondition of Umbilical Cord 收起 << | Phase 2 | Completed | - | Denmark ... 展开 >> Hvidovre Hospital Kettegård Alle 31, Hvidovre, Denmark, 2650 Hvidovre University Hospital Hvidovre, Kettegård alle 30, Denmark, 2650 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.40mL 0.68mL 0.34mL |
16.98mL 3.40mL 1.70mL |
33.97mL 6.79mL 3.40mL |
CAS号 | 550-24-3 |
分子式 | C17H26O4 |
分子量 | 294.386 |
别名 | 恩贝酸/恩贝灵 ;Emberine;NSC 91874;Embelic acid |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 50 mg/mL(169.85 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |