A diterpenoid with diverse biological activities
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Oridonin

Item No. 25665

Technical Information
Formal Name
7,20-epoxy-1α,6β,7α,14R-tetrahydroxy-kaur-16-en-15-one
CAS Number
28957-04-2
Synonyms
  • NSC 250682
Molecular Formula
C20H28O6
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:9): 0.1 mg/mlEthanol: 20 mg/ml
λmax
238 nm
SMILES
O=C1[C@@]2([C@]3([H])O)[C@@]4(O)[C@@H](O)[C@]5([H])C(C)(C)CC[C@H](O)[C@@]5(CO4)[C@]2([H])CC[C@@]3([H])C1=C
InChi Code
InChI=1S/C20H28O6/c1-9-10-4-5-11-18-8-26-20(25,19(11,14(9)22)15(10)23)16(24)13(18)17(2,3)7-6-12(18)21/h10-13,15-16,21,23-25H,1,4-8H2,2-3H3/t10-,11-,12-,13+,15+,16-,18+,19-,20+/m0/s1S
InChi Key
SDHTXBWLVGWJFT-XKCURVIJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Oridonin is a diterpenoid that has been found in R. rubescens and has diverse biological activities.1,2,3 It binds to β-arrestin-1 and -2 (Kds = 362 and 563 nM, respectively) and acts as a modulator by inhibiting β-arrestin recruitment and receptor desensitization and internalization of various G protein-coupled receptors (GPCRs).1 It is selective for β-arrestin over Gαs, Gαq, Gα12, and Gi­­.1 Oridonin also inhibits Akt1 and Akt2 (IC50s = 8.4 and 8.9 µM, respectively).2 Oridonin decreases the proliferation of, and induces cell cycle arrest and apoptosis in, KYSE-70, KYSE-410, and KYSE-450 esophageal cancer cells at 20 µM. Oridonin (40 and 160 mg/kg) reduces tumor growth in a patient-derived xenograft (PDX) mouse model of esophageal squamous cell carcinoma. It is also a covalent inhibitor of NLRP3 inflammasome assembly and activation.3 It reduces plasma, white adipose tissue, and liver levels of IL-1β in wild-type but not Nlrp3-/- mice in a model of high-fat diet-induced type 2 diabetes at 3 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kahsai, A.W., Pakharukova, N., Kwon, H.Y., et alSmall-molecule modulation of β-arrestins. Nature (2026).

    2. Song, M., Liu, X., Liu, K., et alTargeting AKT with oridonin inhibits growth of esophageal squamous cell carcinoma in vitro and patient-derived xenografts in vivo. Mol. Cancer. Ther. 17(7), 1540-1553 (2018).

    3. He, H., Jiang, H., Chen, Y., et alOridonin is a covalent NLRP3 inhibitor with strong anti-inflammasome activity. Nat. Commun. 9(1), 2550 (2018).