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

Chemical Structure : Oridonin

CAS No.: 28957-04-2

Catalog No.: 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.

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50 mg	$88	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	364.438
Formula	C20H28O6
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Kaur-16-en-15-one, 7a,20-epoxy-1a,6b,7,14-tetrahydroxy-, (14R)- (8CI)

References

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.