Oridonin (NSC 250682, Isodonol, β-arrestin inhibitor Cmpd-5)

Chemical Structure : Oridonin

CAS No.: 28957-04-2

加入收藏

货号: PC-35078Not For Human Use, Lab Use Only.

Oridonin (NSC 250682, Isodonol, β-arrestin inhibitor Cmpd-5) is a high-affinity NLRP3 inflammasome inhibitor (Kd=52.5 nM), covalently binds within NACHT domain, blocks interaction of NLRP3 with NEK.

规格	价格	库存
25 mg	￥580	In stock
50 mg	￥880	In stock
100 mg	￥1280	In stock
250 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

Oridonin (NSC 250682, Isodonol, β-arrestin inhibitor Cmpd-5) is a high-affinity NLRP3 inflammasome inhibitor (Kd=52.5 nM), covalently binds within NACHT domain, blocks interaction of NLRP3 with NEK.

Oridonin (NSC 250682, Isodonol, β-arrestin inhibitor Cmpd-5) also is an inhibitor of AKT with IC50s of 8.4 and 8.9 μM for AKT1 and AKT2 respectively.

Oridonin (NSC 250682, Isodonol, β-arrestin inhibitor Cmpd-5) also is a small-molecule β-arrestin inhibitor with ITC Kd of 362 nM and 563 nM for βARR1 and βARR2 respectively.

Cmpd-5 inhibits ERK signalling, impair T cell migration and blunt β-arrestin-mediated cardiomyocyte contractility.

Cmpd-5 binds the MCL site in βARR1 and engages a structurally dynamic interface.

Oridonin is an active diterpenoid compound isolated from the plant Rabdosia Rrubescens, has various pharmacological activities, including antioxidant, anti-tumor capacities and anti-inflammation.

Oridonin interacts with the ATP-binding pocket of AKT, inhibits growth of ESCC in vitro and patient derived xenografts in vivo.

Oridonin inhibits vascular inflammation by blocking NF-κB and MAPK activation.

物理化学性质&存储条件

分子量	364.438
分子式	C20H28O6
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Kaur-16-en-15-one, 7a,20-epoxy-1a,6b,7,14-tetrahydroxy-, (14R)- (8CI)

参考文献

1. Song M, et al. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0823.2017.

2. Kadioglu O, et al. Front Pharmacol. 2018 Apr 16;9:355.

3. Huang W, et al. Eur J Pharmacol. 2018 May 5;826:133-139.

4. Zhang HP, et al. Oncotarget. 2017 Oct 16;8(63):106833-106843.