Oridonin (Synonyms: NSC-250682; Isodonol)

Name: Oridonin
Brand: MedChemExpress
SKU: HY-N0004
Rating: 5.0 (26 reviews)

Cat. No.: HY-N0004 Purity: 99.89%: Data Sheet
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Oridonin (NSC-250682), a diterpenoid isolated from Rabdosia rubescens, acts as an inhibitor of AKT, with IC₅₀s of 8.4 and 8.9 μM for AKT1 and AKT2; Oridonin possesses anti-tumor, anti-bacterial and anti-inflammatory effects.

For research use only. We do not sell to patients.

CAS No. : 28957-04-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 26 publication(s) in Google Scholar

Other Forms of Oridonin:

Oridonin (Standard) Get quote

26 Publications Citing Use of MCE Oridonin

ELISA

In Vivo Efficacy Study

Bio/Physico-chemical Assay

: Oridonin purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 May 27;16(1):4887.; Oridonin (0.5-2.5 µM; 11 h). NLRP3-KO iBMDMs were stimulated with LPS and Dox after a 30-min pre-incubation with inhibitors or DMSO, except for Ctrl, where only LPS was added. Measurements of IL-1β were normalized to “LPS/Dox”- treated WT^R258W.

: Oridonin purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2025 May 28;82(1):218. [Abstract]; CD3/CD28 mAbs-stimulated lymphocytes were treated with AKT inhibitor Oridonin (10 μM) or not. Western blot showing the expression of indicated molecules at 3 h.

: Oridonin purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Apr;44(4):726-740. [Abstract]; Oridonin (Ori; 5-20 mg/kg; ip). The infarct volume was determined by conducting TTC staining at 1 d after reperfusion. Representative TTC-stained brain slices of different groups are shown.

: Oridonin purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2023 Apr;44(4):726-740. [Abstract]; Oridonin (Ori; 5-20 mg/kg; ip). The expression levels of Bax, Bcl-2, mitochondrial Cyto-C, cytoplasmic Cyto-C, caspase-3 and cleaved caspase-3 were measured by Western blot analysis in the ipsilateral brain region at 1 d after reperfusion.

: Oridonin purchased from MedChemExpress. Usage Cited in: Cell Mol Life Sci. 2021 Dec 31;79(1):27. [Abstract]; Time-dependent PHGDH inhibition. Samples of 200 nM PHGDH were pre-incubated with 1 μM Oridonin for the indicated times, and then PHGDH activity was monitored for 5 h. The time line is shown above. Black arrow indicates the start of the reaction. The data are normalized to the 5 h reading of the ‘0 min’ pre-incubated enzyme.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

Akt1

8.4 μM (IC₅₀)

Akt2

8.9 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	10.4 μM Compound: 1	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27089099]
A549	IC₅₀	13.45 μM Compound: Oridonin	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31494472]
A549	IC₅₀	17.8 μM Compound: 1	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
A549	IC₅₀	18.15 μM Compound: 1	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30921757]
A549	IC₅₀	18.7 μM Compound: Oridonin	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 26115572]
A549	IC₅₀	25.4 μM Compound: Oridonin	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30193221]
A549	IC₅₀	26.15 μM Compound: Oridonin	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 22483090]
A549	IC₅₀	27.24 μM Compound: 1	Cytotoxicity against human A549 cells by MTT assay Cytotoxicity against human A549 cells by MTT assay	[PMID: 18644718]
A549	IC₅₀	30.4 μM Compound: 1; ORI	Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 cells Antiproliferative activity against human A549 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
A549	IC₅₀	7.2 μM Compound: 4	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 25590529]
A549	IC₅₀	> 10 μM Compound: 18	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 20521771]
A549	IC₅₀	> 10 μM Compound: 20	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 23819871]
B16	IC₅₀	24.89 μM Compound: 1	Antiproliferative activity against mouse B16 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against mouse B16 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
B16	IC₅₀	26.15 μM Compound: 1	Cytotoxicity against mouse B16 cells by MTT assay Cytotoxicity against mouse B16 cells by MTT assay	[PMID: 18644718]
Bel-7402	IC₅₀	39.8 μM Compound: 1	Cytotoxicity against human BEL-7402 cells by MTT assay Cytotoxicity against human BEL-7402 cells by MTT assay	[PMID: 18644718]
Bel-7402	IC₅₀	5.41 μM Compound: 1	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 28165738]
Bel-7402	IC₅₀	7.12 μM Compound: 1	Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human Bel-7402 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27158140]
Bel-7402	IC₅₀	7.36 μM Compound: 1	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 29407983]
Bel-7402	IC₅₀	7.48 μM Compound: 1	Anticancer activity against human Bel7402 cells assessed as growth inhibition by MTT assay Anticancer activity against human Bel7402 cells assessed as growth inhibition by MTT assay	[PMID: 25050168]
Bel-7402	IC₅₀	7.48 μM Compound: 1	Antiproliferative activity against human Bel7402 cells assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25050168]
Bel-7402	IC₅₀	7.48 μM Compound: 9	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 23644204]
Bel-7402	IC₅₀	7.48 μM Compound: Oridonin	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 22483090]
Bel-7402	IC₅₀	7.48 μM Compound: Oridonin	Antiproliferative activity against human Bel7402 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human Bel7402 cells assessed as growth inhibition by MTT assay	[PMID: 23274570]
Bel-7402	IC₅₀	7.56 μM Compound: 7	Antiproliferative activity against human Bel7402 cells after 24 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 24 hrs by MTT assay	[PMID: 27491707]
Bel-7402	IC₅₀	7.85 μM Compound: 1	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30921757]
Bel-7402	IC₅₀	8.31 μM Compound: 1	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
Bel-7402	IC₅₀	9.59 μM Compound: Oridonin	Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human Bel7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30981113]
Bel-7402	IC₅₀	> 10 μM Compound: 1	Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 28901767]
Bel7402/5-FU	IC₅₀	10.51 μM Compound: 1	Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by MTT assay Antiproliferative activity against human Bel7402/5-FU cells after 72 hrs by MTT assay	[PMID: 29407983]
DU-4475	IC₅₀	16.95 μM Compound: 1	Antiproliferative activity against human DU4475 cells after 72 hrs by MTT assay Antiproliferative activity against human DU4475 cells after 72 hrs by MTT assay	[PMID: 32610904]
EC9706	IC₅₀	38.42 μM Compound: Oridonin	Antiproliferative activity against human EC9706 cells after 48 hrs by MTT assay Antiproliferative activity against human EC9706 cells after 48 hrs by MTT assay	[PMID: 30143365]
H22	IC₅₀	4.88 μM Compound: 1	Antiproliferative activity against mouse H22 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against mouse H22 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
HCC1806	IC₅₀	21.74 μM Compound: 1	Antiproliferative activity against human HCC1806 cells after 72 hrs by MTT assay Antiproliferative activity against human HCC1806 cells after 72 hrs by MTT assay	[PMID: 32610904]
HCC1937	IC₅₀	8.27 μM Compound: 1	Antiproliferative activity against human HCC1937 cells after 72 hrs by MTT assay Antiproliferative activity against human HCC1937 cells after 72 hrs by MTT assay	[PMID: 32610904]
HCT-116	IC₅₀	11.73 μM Compound: 1	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
HCT-116	IC₅₀	6.84 μM Compound: Oridonin	Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30981113]
HCT-116	IC₅₀	6.84 μM Compound: Oridonin	Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by MTS assay Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability by MTS assay	[PMID: 38107170]
HEK-293T	IC₅₀	> 5 μM Compound: 23	Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay Cytotoxicity against human 293T cells assessed as cell viability by dual-luciferase reporter assay	[PMID: 21393004]
HEp-2	EC₅₀	37.1 μM Compound: 1	Anticancer activity against human Hep2 cells measured after 24 hrs by MTT assay Anticancer activity against human Hep2 cells measured after 24 hrs by MTT assay	[PMID: 27344488]
HEp-2	IC₅₀	37.1 μM Compound: 1	Cytotoxicity against human Hep2 cells after 24 hrs by MTT assay Cytotoxicity against human Hep2 cells after 24 hrs by MTT assay	[PMID: 20496901]
HGC-27	IC₅₀	32.03 μM Compound: Oridonin	Antiproliferative activity against human HGC27 cells after 48 hrs by MTT assay Antiproliferative activity against human HGC27 cells after 48 hrs by MTT assay	[PMID: 30143365]
HL-60	IC₅₀	14.3 μM Compound: 1	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay	[PMID: 29407983]
HL-60	IC₅₀	2.5 μM Compound: 20	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 23819871]
HL-60	IC₅₀	3.9 μM Compound: 18	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 20521771]
HL-60	IC₅₀	32.76 μM Compound: 1	Cytotoxicity against human HL60 cells by MTT assay Cytotoxicity against human HL60 cells by MTT assay	[PMID: 18644718]
HL-60	IC₅₀	7.2 μM Compound: 4	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay Cytotoxicity against human HL60 cells after 48 hrs by MTT assay	[PMID: 25590529]
HL-60	IC₅₀	9.46 μM Compound: 1	Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30921757]
HMEC	IC₅₀	5.6 μM Compound: 1	Growth inhibition of human HMEC cells after 48 hrs Growth inhibition of human HMEC cells after 48 hrs	[PMID: 24128046]
HMEC-1	IC₅₀	> 4 μg/mL Compound: 2	Cytotoxicity against HMEC1 cells by resazurin assay Cytotoxicity against HMEC1 cells by resazurin assay	[PMID: 14738375]
HSC-T6	EC₅₀	7 μM Compound: 1	Anticancer activity against rat HSC-T6 cells measured after 48 hrs by alamar blue assay Anticancer activity against rat HSC-T6 cells measured after 48 hrs by alamar blue assay	[PMID: 27344488]
HeLa	IC₅₀	17.28 μM Compound: 1	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
HeLa	IC₅₀	17.8 μM Compound: 1	Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27089099]
HeLa	IC₅₀	32.7 μM Compound: Oridonin	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 22483090]
HepG2	IC₅₀	15.2 μM Compound: 1	Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27089099]
HepG2	IC₅₀	3.66 μM Compound: Oridonin	Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 21144747]
HepG2	IC₅₀	8.12 μM Compound: 1; ORI	Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 cells Antiproliferative activity against human HepG2 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
HepG2	IC₅₀	8.95 μM Compound: 1	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
Jurkat	EC₅₀	1.2 μM Compound: 1	Anticancer activity against human Jurkat cells measured after 48 hrs by trypan blue assay Anticancer activity against human Jurkat cells measured after 48 hrs by trypan blue assay	[PMID: 27344488]
K562	EC₅₀	14.6 μM Compound: 1	Anticancer activity against human K562 cells measured after 24 hrs by MTT assay Anticancer activity against human K562 cells measured after 24 hrs by MTT assay	[PMID: 27344488]
K562	EC₅₀	4.76 μM Compound: 1	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 27344488]
K562	IC₅₀	4.25 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 36037626]
K562	IC₅₀	4.32 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
K562	IC₅₀	4.33 μM Compound: 1	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 28165738]
K562	IC₅₀	4.57 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
K562	IC₅₀	4.59 μM Compound: 7	Antiproliferative activity against human K562 cells after 24 hrs by MTT assay Antiproliferative activity against human K562 cells after 24 hrs by MTT assay	[PMID: 27491707]
K562	IC₅₀	4.64 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30921757]
K562	IC₅₀	4.76 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25050168]
K562	IC₅₀	4.76 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27089099]
K562	IC₅₀	4.76 μM Compound: 9	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 23644204]
K562	IC₅₀	4.76 μM Compound: Oridonin	Cytotoxicity against human K562 cells after 72 hrs by MTT assay Cytotoxicity against human K562 cells after 72 hrs by MTT assay	[PMID: 22483090]
K562	IC₅₀	4.76 μM Compound: Oridonin	Antiproliferative activity against human K562 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human K562 cells assessed as growth inhibition by MTT assay	[PMID: 23274570]
K562	IC₅₀	4.79 μM Compound: 1	Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
K562	IC₅₀	5.1 μM Compound: 1	Antiproliferative activity against human K562 cells after 72 hrs by MTT assay Antiproliferative activity against human K562 cells after 72 hrs by MTT assay	[PMID: 28901767]
K562/Adr	EC₅₀	< 40 μM Compound: 1	Anticancer activity against human K562/ADR cells measured after 24 hrs by MTT assay Anticancer activity against human K562/ADR cells measured after 24 hrs by MTT assay	[PMID: 27344488]
KB 3-1	IC₅₀	13.24 μM Compound: 1	Antiproliferative activity against human KB-3-1 cells after 48 hrs by MTT assay Antiproliferative activity against human KB-3-1 cells after 48 hrs by MTT assay	[PMID: 28165738]
Kasumi 1	EC₅₀	1.33 μM Compound: 1	Anticancer activity against human Kasumi-1 cells measured after 48 hrs by CCK8 assay Anticancer activity against human Kasumi-1 cells measured after 48 hrs by CCK8 assay	[PMID: 27344488]
L02	IC₅₀	17.47 μM Compound: 1; ORI	Cytotoxicity against human LO2 cells incubated for 72 hrs by CCK8 cells Cytotoxicity against human LO2 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
L02	IC₅₀	17.78 μM Compound: 1	Cytotoxicity against human L02 cells by MTT assay Cytotoxicity against human L02 cells by MTT assay	[PMID: 25050168]
L02	IC₅₀	18.68 μM Compound: 1	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
L02	IC₅₀	18.94 μM Compound: 1	Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay	[PMID: 29407983]
L02	IC₅₀	19.53 μM Compound: 1	Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30921757]
L02	IC₅₀	21.59 μM Compound: 1	Cytotoxicity against human L02 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human L02 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 31877536]
L02	IC₅₀	25.01 μM Compound: 1	Cytotoxicity against human L02 cells incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells incubated for 72 hrs by MTT assay	[PMID: 36037626]
L02	IC₅₀	34.32 μM Compound: 1	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
L02	IC₅₀	38.2 μM Compound: Ori	Cytotoxicity against human L-02 cells incubated for 24 hrs by MTT assay Cytotoxicity against human L-02 cells incubated for 24 hrs by MTT assay	[PMID: 34506712]
L02	IC₅₀	42.25 μM Compound: Oridonin	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 35428012]
L02	IC₅₀	6.97 μM Compound: Oridonin	Cytotoxicity in human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in human L02 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30981113]
LNCaP	EC₅₀	25 μM Compound: 1	Anticancer activity against human LNCAP cells measured after 48 hrs by CCK8 assay Anticancer activity against human LNCAP cells measured after 48 hrs by CCK8 assay	[PMID: 27344488]
MCF7	EC₅₀	4.4 μM Compound: 1	Antiproliferative activity against human ER-positive MCF7 cells measured after 48 hrs by MTT assay Antiproliferative activity against human ER-positive MCF7 cells measured after 48 hrs by MTT assay	[PMID: 27344488]
MCF7	EC₅₀	6.6 μM Compound: 1	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 27344488]
MCF7	IC₅₀	11.11 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
MCF7	IC₅₀	13.85 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 31877536]
MCF7	IC₅₀	14.6 μM Compound: 1	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25050168]
MCF7	IC₅₀	14.6 μM Compound: Oridonin	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 22483090]
MCF7	IC₅₀	17.56 μM Compound: Oridonin	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 30981113]
MCF7	IC₅₀	17.89 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28165738]
MCF7	IC₅₀	21.97 μM Compound: Oridonin	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31494472]
MCF7	IC₅₀	21.97 μM Compound: Oridonin	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 32883640]
MCF7	IC₅₀	4.36 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 24128046]
MCF7	IC₅₀	6.6 μM Compound: 126	Antiproliferative activity against ER-positive human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against ER-positive human MCF7 cells after 48 hrs by MTT assay	[PMID: 35033884]
MCF7	IC₅₀	6.72 μM Compound: 13	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29528645]
MCF7	IC₅₀	64.3 μM Compound: Oridonin	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30193221]
MCF7	IC₅₀	7.2 μM Compound: 4	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 25590529]
MCF7	IC₅₀	74.18 μM Compound: Oridonin	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 30143365]
MCF7	IC₅₀	9.1 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 28901767]
MCF7	IC₅₀	> 10 μM Compound: 20	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 23819871]
MDA-MB-231	EC₅₀	28 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay	[PMID: 27344488]
MDA-MB-231	EC₅₀	29.4 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells Antiproliferative activity against human MDA-MB-231 cells	[PMID: 27344488]
MDA-MB-231	EC₅₀	29.4 μM Compound: Oridonin	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay	[PMID: 30981113]
MDA-MB-231	IC₅₀	11.62 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
MDA-MB-231	IC₅₀	11.68 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 36037626]
MDA-MB-231	IC₅₀	17.92 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 32610904]
MDA-MB-231	IC₅₀	2.38 μM Compound: Oridonin	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 21144747]
MDA-MB-231	IC₅₀	28 μM Compound: 1	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 24128046]
MDA-MB-231	IC₅₀	29.4 μM Compound: 13	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 29528645]
MDA-MB-453	IC₅₀	6.67 μM Compound: 1	Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by MTT assay	[PMID: 32610904]
MDA-MB-468	EC₅₀	5.3 μM Compound: 1	Antiproliferative activity against human ER-triple negative MDA-MB-468 cells measured after 48 hrs by MTT assay Antiproliferative activity against human ER-triple negative MDA-MB-468 cells measured after 48 hrs by MTT assay	[PMID: 27344488]
MDA-MB-468	IC₅₀	17.28 μM Compound: 1	Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 cells after 72 hrs by MTT assay	[PMID: 32610904]
MGC-803	EC₅₀	5.69 μM Compound: 1	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 27344488]
MGC-803	IC₅₀	14.13 μM Compound: Oridonin	Antiproliferative activity against human MGC803 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human MGC803 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31494472]
MGC-803	IC₅₀	14.13 μM Compound: Oridonin	Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 32883640]
MGC-803	IC₅₀	15.11 μM Compound: 1	Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
MGC-803	IC₅₀	3.57 μM Compound: Oridonin	Cytotoxicity against human MGC803 cells after 48 hrs by MTT assay Cytotoxicity against human MGC803 cells after 48 hrs by MTT assay	[PMID: 21144747]
MGC-803	IC₅₀	33.1 μM Compound: Oridonin	Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 48 hrs by MTT assay	[PMID: 30143365]
MGC-803	IC₅₀	34.3 μM Compound: Oridonin	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 30193221]
MGC-803	IC₅₀	4.5 μM Compound: 1	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 28901767]
MGC-803	IC₅₀	5.47 μM Compound: 7	Antiproliferative activity against human MGC803 cells after 24 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 24 hrs by MTT assay	[PMID: 27491707]
MGC-803	IC₅₀	5.69 μM Compound: 1	Antiproliferative activity against human MGC803 cells assessed as growth inhibition after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 25050168]
MGC-803	IC₅₀	5.69 μM Compound: 9	Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 23644204]
MGC-803	IC₅₀	5.69 μM Compound: Oridonin	Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay Cytotoxicity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 22483090]
MGC-803	IC₅₀	5.69 μM Compound: Oridonin	Antiproliferative activity against human MGC803 cells assessed as growth inhibition by MTT assay Antiproliferative activity against human MGC803 cells assessed as growth inhibition by MTT assay	[PMID: 23274570]
MGC-803	IC₅₀	9.06 μM Compound: 1	Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay Antiproliferative activity against human MGC803 cells after 72 hrs by MTT assay	[PMID: 28165738]
MT2	EC₅₀	1.2 μM Compound: 1	Anticancer activity against human MT2 cells measured after 48 hrs by trypan blue assay Anticancer activity against human MT2 cells measured after 48 hrs by trypan blue assay	[PMID: 27344488]
NCI-H460	IC₅₀	17.14 μM Compound: 1	Anticancer activity against human NCI-H460 cells by MTT assay Anticancer activity against human NCI-H460 cells by MTT assay	[PMID: 25050168]
NCI-H460	IC₅₀	20.51 μM Compound: 1	Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 48 hrs by MTT assay	[PMID: 28165738]
NCI/ADR-RES	EC₅₀	34.8 μM Compound: 1	Antiproliferative activity against human MCF7/ADR cells measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7/ADR cells measured after 48 hrs by MTT assay	[PMID: 27344488]
NCI/ADR-RES	IC₅₀	26.18 μM Compound: 1	Antiproliferative activity against human MCF7/ADR cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7/ADR cells after 72 hrs by MTT assay	[PMID: 32610904]
NCI/ADR-RES	IC₅₀	> 30 μM Compound: 1	Growth inhibition of human MCF7/ADR cells after 48 hrs Growth inhibition of human MCF7/ADR cells after 48 hrs	[PMID: 24128046]
PANC-1	IC₅₀	> 10 μM Compound: 18	Growth inhibition of human PANC1 cells after 48 hrs by SRB assay Growth inhibition of human PANC1 cells after 48 hrs by SRB assay	[PMID: 20521771]
PBMC	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PBMC assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
PBMC	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against human PBMC cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human PBMC cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 31877536]
PC-3	EC₅₀	25 μM Compound: 1	Anticancer activity against human PC3 cells measured after 48 hrs by CCK8 assay Anticancer activity against human PC3 cells measured after 48 hrs by CCK8 assay	[PMID: 27344488]
PC-3	IC₅₀	10.07 μM Compound: 1	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30921757]
PC-3	IC₅₀	10.97 μM Compound: 1	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29407983]
PC-3	IC₅₀	27.55 μM Compound: Oridonin	Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against human PC3 cells after 48 hrs by MTT assay	[PMID: 30143365]
PC-3	IC₅₀	43.9 μM Compound: Oridonin	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 30193221]
PLC-PRF-5	IC₅₀	7.41 μM Compound: 1; ORI	Antiproliferative activity against human PLC/PRF/5 cells incubated for 72 hrs by CCK8 cells Antiproliferative activity against human PLC/PRF/5 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
Panel NCI-60 (60 carcinoma cell lines)	GI₅₀	453 nM Compound: Oridonin	Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program Growth inhibitory activity against human cancer cell line in the NCI's anticancer drug screening program	[PMID: 15743190]
RAW264.7	IC₅₀	5.2 μM Compound: 20	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method	[PMID: 23819871]
RPMI-8226	EC₅₀	1.2 μM Compound: 1	Anticancer activity against human RPMI8226 cells measured after 48 hrs by trypan blue assay Anticancer activity against human RPMI8226 cells measured after 48 hrs by trypan blue assay	[PMID: 27344488]
RPMI-8226	IC₅₀	9.25 μM Compound: 1; ORI	Antiproliferative activity against human RPMI8226 cells incubated for 72 hrs by CCK8 cells Antiproliferative activity against human RPMI8226 cells incubated for 72 hrs by CCK8 cells	[PMID: 31200238]
SGC-7901	IC₅₀	7.13 μM Compound: 1	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30921757]
SGC-7901	IC₅₀	7.87 μM Compound: 1	Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human SGC7901 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31202992]
SK-BR-3	IC₅₀	8.49 μM Compound: 1	Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 cells after 72 hrs by MTT assay	[PMID: 32610904]
SK-BR-3	IC₅₀	> 10 μM Compound: 18	Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay Cytotoxicity against human SK-BR-3 cells after 48 hrs by MTT assay	[PMID: 20521771]
SMMC-7721	IC₅₀	12.57 μM Compound: 1	Antiproliferative activity against human SMMC-7221 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human SMMC-7221 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
SMMC-7721	IC₅₀	14.41 μM Compound: 1	Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 36037626]
SMMC-7721	IC₅₀	30.1 μM Compound: Oridonin	Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay Antiproliferative activity against human SMMC7721 cells after 72 hrs by MTT assay	[PMID: 30193221]
SMMC-7721	IC₅₀	53.95 μM Compound: Oridonin	Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay Antiproliferative activity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 30143365]
SMMC-7721	IC₅₀	7.2 μM Compound: 4	Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 25590529]
SMMC-7721	IC₅₀	> 10 μM Compound: 18	Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 20521771]
SMMC-7721	IC₅₀	> 10 μM Compound: 20	Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 48 hrs by MTT assay	[PMID: 23819871]
SW-620	EC₅₀	20.8 μM Compound: 1	Anticancer activity against human SW620 cells measured after 24 hrs by MTT assay Anticancer activity against human SW620 cells measured after 24 hrs by MTT assay	[PMID: 27344488]
SW-620	IC₅₀	4.67 μM Compound: 1	Anticancer activity against ABCB1-overexpressing human SW620/AD300 cells by MTT assay Anticancer activity against ABCB1-overexpressing human SW620/AD300 cells by MTT assay	[PMID: 25050168]
SW-620	IC₅₀	6.26 μM Compound: 1	Anticancer activity against human SW620 cells by MTT assay Anticancer activity against human SW620 cells by MTT assay	[PMID: 25050168]
SW480	EC₅₀	20.8 μM Compound: 1	Anticancer activity against human SW480 cells measured after 24 hrs by MTT assay Anticancer activity against human SW480 cells measured after 24 hrs by MTT assay	[PMID: 27344488]
SW480	IC₅₀	10.59 μM Compound: 1	Antiproliferative activity against human SW480 cells assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 36037626]
SW480	IC₅₀	11.63 μM Compound: 1	Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]
SW480	IC₅₀	31.42 μM Compound: 1	Cytotoxicity against human SW480 cells by MTT assay Cytotoxicity against human SW480 cells by MTT assay	[PMID: 18644718]
SW480	IC₅₀	7.2 μM Compound: 4	Cytotoxicity against human SW480 cells after 48 hrs by MTT assay Cytotoxicity against human SW480 cells after 48 hrs by MTT assay	[PMID: 25590529]
SW480	IC₅₀	> 10 μM Compound: 20	Cytotoxicity against human SW480 cells after 48 hrs by MTT assay Cytotoxicity against human SW480 cells after 48 hrs by MTT assay	[PMID: 23819871]
T47D	IC₅₀	7.56 μM Compound: 1	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay Antiproliferative activity against human T47D cells after 72 hrs by MTT assay	[PMID: 32610904]
TE-1	IC₅₀	12.73 μM Compound: Oridonin	Antiproliferative activity against human TE1 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay Antiproliferative activity against human TE1 cells assessed as reduction in cell viability incubated for 72 hrs by SRB assay	[PMID: 31494472]
TE-1	IC₅₀	12.73 μM Compound: Oridonin	Antiproliferative activity against human TE-1 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay Antiproliferative activity against human TE-1 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	[PMID: 32883640]
THP-1	CC₅₀	19.8 μM Compound: Oridonin	Cytotoxicity against human THP-1 cells by CCK-8 method Cytotoxicity against human THP-1 cells by CCK-8 method	[PMID: 38244941]
U-266	EC₅₀	1.2 μM Compound: 1	Anticancer activity against human U266 cells measured after 48 hrs by trypan blue assay Anticancer activity against human U266 cells measured after 48 hrs by trypan blue assay	[PMID: 27344488]
U-87MG ATCC	IC₅₀	14.05 μM Compound: 1	Antiproliferative activity against human U-87 MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human U-87 MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 35121201]

In Vitro

Oridonin is an ATP-competitive inhibitor of AKT with IC₅₀s of 8.4 and 8.9 μM for AKT1 and AKT2, respectively. Oridonin (5, 10 or 20 μM) obviously inhibits the growth of KYSE70, KYSE410 and KYSE450 ESCC cells via targeting AKT1/2. Oridonin (10 or 20 μM) causes G2/M phase cell cycle arrest in KYSE70, KYSE410 and KYSE450 cells, and induces apoptosis in these three cell lines at 20 μM. In addition, Oridonin (5, 10 or 20 μM) in combination with cisplatin or 5-FU enhances the inhibition of esophageal squamous cell carcinoma (ESCC) cell growth^[1]. Oridonin (0.1 and 1 μM) preferentially suppresses AKT/mTOR signaling. Oridonin (1 μM) also selectively suppresses growth of breast cancer cells with hyperactivation of AKT signaling^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oridonin (160 mg/kg, p.o.) shows significant reduction in the tumor growth without obvious weigh loss in SCID mice bearing EG9 and HEG18 tumor cells. Oridonin treatment also suppresses the expression of Ki-67, phosphorylated AKT, GSK-3β or mTOR in mice^[1]. Oridonin (15 mg/kg, i.p.) impairs cell growth in breast cancer with hyperactivation of AKT signaling in nude mice^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

364.43

Formula

C₂₀H₂₈O₆

CAS No.

28957-04-2

Appearance

Solid

Color

White to off-white

SMILES

O[C@@H]1[C@]2(CO3)[C@@]([C@H](O)[C@]3(O)[C@]45[C@@]2([H])CC[C@](C(C5=O)=C)([H])[C@@]4([H])O)([H])C(C)(C)CC1

Structure Classification

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 62.5 mg/mL (171.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7440 mL	13.7201 mL	27.4401 mL
5 mM	0.5488 mL	2.7440 mL	5.4880 mL
10 mM	0.2744 mL	1.3720 mL	2.7440 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% 1-Methyl-2-pyrrolidinone 90% PEG300
Solubility: ≥ 5 mg/mL (13.72 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (327 KB) SDS (396 KB)

COA (263 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Song M, et al. Targeting AKT with oridonin inhibits growth of esophageal squamous cell carcinoma in vitro and patient derived xenografts in vivo. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0823.2017. [Content Brief]

[2]. Sun B, et al. Oridonin inhibits aberrant AKT activation in breast cancer. Oncotarget. 2018 Feb 1;9(35):23878-23889. [Content Brief]

Kinase Assay ^[1]	For the AKT kinase assay, the ADP-Glo™ Kinase Assay Kit is used. Active AKT1 or AKT2 kinase and inactive GSK-3β as substrate are mixed by 1× reaction buffer and then added to a white 96-well plate. Pure ATP provided in the kit is serially diluted obtain a final concentration of 0, 1, 10, 50, and 100 μM. GSK-3β is added to reach a final concentration of 2.5, 5, 10 or 20 μM and DMSO is used as a control. The mixed solution is incubated at room temperature and luciferase activity is measured using the Luminoskan Ascent plate reader^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Cells are seeded (6×10³ cells/well for KYSE70; 2.5×10³ cells/well for KYSE410; 2×10³ cells/well for KYSE450) in 96-well plates and incubated for 24 h and then treated with different amounts of Oridonin or vehicle. After incubation for 24, 48 or 72 h, cell proliferation is measured by the MTT assay. For anchorage-independent cell growth assessment, cells (2.5, 5 or 10 μM Oridonin) suspended in complete medium are added to 0.3% agar with vehicle, 2.5, 5 or 10 μM Oridonin in a top layer over a base layer of 0.5% agar with vehicle, 2.5, 5 or 10 μM Oridonin. The cultures are maintained at 37°C in a 5% CO₂ incubator for 3 weeks and then colonies are visualized under a microscope and counted using the Image-Pro Plus software program^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Mice^[2] Breast cancer cells are harvested and resuspended in 40% Matrigel-Basement Membrane Matrix, LDEV-free, and then injected (100 μL per site) into the fourth pair of mammary fat pads of nude mice (CrTac: NCr-Foxn1nu). Tumors are measured in two dimensions using manual calipers. Tumor volume is calculated using the formula: Volume = 0.5 × length × width × width. Tumor volume is measured every 2-3 days. Upon harvesting, tumors are fixed in formalin overnight and then in 70% ethanol for histopathology analysis. Mice are treated with Oridonin (15 mg/kg) in 1% Pluronic F68 or vehicle (1% Pluronic F68) daily by intraperitoneal (IP) injection. BEZ235 is reconstituted 1:9 in 1-methyl-2 pyrolidone and polyethylene glycol 300 (PEG300) Mice are treated with this compound formulation at 45 mg/kg daily (QD) by oral gavage^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Song M, et al. Targeting AKT with oridonin inhibits growth of esophageal squamous cell carcinoma in vitro and patient derived xenografts in vivo. Mol Cancer Ther. 2018 Apr 25. pii: molcanther.0823.2017. [Content Brief] [2]. Sun B, et al. Oridonin inhibits aberrant AKT activation in breast cancer. Oncotarget. 2018 Feb 1;9(35):23878-23889. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7440 mL	13.7201 mL	27.4401 mL	68.6003 mL
	5 mM	0.5488 mL	2.7440 mL	5.4880 mL	13.7201 mL
	10 mM	0.2744 mL	1.3720 mL	2.7440 mL	6.8600 mL
	15 mM	0.1829 mL	0.9147 mL	1.8293 mL	4.5734 mL
	20 mM	0.1372 mL	0.6860 mL	1.3720 mL	3.4300 mL
	25 mM	0.1098 mL	0.5488 mL	1.0976 mL	2.7440 mL
	30 mM	0.0915 mL	0.4573 mL	0.9147 mL	2.2867 mL
	40 mM	0.0686 mL	0.3430 mL	0.6860 mL	1.7150 mL
	50 mM	0.0549 mL	0.2744 mL	0.5488 mL	1.3720 mL
	60 mM	0.0457 mL	0.2287 mL	0.4573 mL	1.1433 mL
	80 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8575 mL
	100 mM	0.0274 mL	0.1372 mL	0.2744 mL	0.6860 mL

Oridonin Related Classifications

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Oridonin28957-04-2NSC-250682 IsodonolNSC250682NSC 250682AktBacterialLigands for E3 LigasePKBProtein kinase BE3 ligase-recruiting MoietyInhibitorinhibitorinhibit

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Oridonin (Synonyms: NSC-250682; Isodonol)

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