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Fig. 1 · Structure
Cat. No.
A10889
CAS No.
568-73-0
Formula
C18H12O3
Mol. Weight
276.3

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Tanshinone I

Cat. No. A10889 CAS 568-73-0

Phospholipase inhibitor

Tanshinones are the major bioactive compounds of Salvia miltiorrhiza Bunge (Danshen) roots, which are used in many therapeutic remedies in Chinese traditional medicine.

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Publications for Tanshinone I

1 publication citing this product

  1. Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125
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For laboratory research use only. We do not sell to patients.

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Biological Activity

Bioactivity / Mechanism

Tanshinone I bound immobilized zebrafish EZH2 in an SPR assay (reported KD 29.379 µM) and inhibited PRC2-mediated H3K27 methylation in a separate biochemical assay. These results do not establish broad target selectivity. [1]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Target & Activity

Target Activity Value
PLA2 11 μM

Cellular Effect

Cell Line Activity Value Description Reference
AGS IC50 > 50 μM Viability of human AGS cells under normoxic conditions after 24 hrs by MTT assay [PMID: 17583950]
AGS IC50 12.5 μM Inhibition of HIF1 activation in human AGS cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay [PMID: 17583950]
Hep 3B2 EC50 > 10 μM Cytotoxicity against human Hep3B cells deficient in p53 gene by MTT assay [PMID: 20455578]
Hep 3B2 IC50 > 50 μM Viability of human Hep3B cells under normoxic conditions after 24 hrs by MTT assay [PMID: 17583950]
Hep 3B2 IC50 8.51 μM Inhibition of HIF1 activation in human Hep3B cells assessed as inhibition of hypoxia-induced luciferase expression after 16 hrs by reporter assay [PMID: 17583950]
HepG2 EC50 > 10 μM Cytotoxicity against doxorubicin resistant human HepG2 cells expressing wild type p53 gene by MTT assay [PMID: 20455578]
HepG2 EC50 6.3 μM Cytotoxicity against human HepG2 cells expressing wild type p53 gene by MTT assay [PMID: 20455578]
KB IC50 5.87 μM Antiproliferative activity against human KB cells after 72 hrs by sulforhodamine B assay [PMID: 29294282]
MCF7 IC50 7.927 μM Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay [PMID: 33751939]
MDA-MB-231 IC50 7.962 μM Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 24 hrs by MTT assay [PMID: 33751939]
MIA PaCa-2 IC50 10.5 μM Cytotoxicity against human MIAPaCa2 cells after 24 hrs by MTT assay [PMID: 21775156]
PLC-PRF-5 EC50 > 10 μM Cytotoxicity against human PLC/PRF/5 cells expressing mutant p53 gene (codon 249) by MTT assay [PMID: 20455578]
Vero C1008 CC50 > 200 μM Cytotoxicity against African green monkey Vero E6 cells assessed as cell viability treated for 24 hrs by CCK8 assay [PMID: 35620927]

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In Vitro Studies

In H1299 cells, Aurora A silencing reduced proliferation and attenuated the additional antiproliferative effect of tanshinone I, supporting a role for Aurora A in the cellular response. [2]

Binding to immobilized zebrafish EZH2

Biochemical assay · Recombinant zebrafish EZH2; SPR [1]

Concentration-dependent binding was measured by SPR. The binding site and broader selectivity remain unresolved.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tan I–zebrafish EZH2 bindingKD 29.379 µM[1]

Literature-Reported Treatment Conditions

Treatment concentration
0.78, 1.56, 3.125, 6.25, 12.5, 25, 50 µM
Exposure duration
2 min contact; 2 min dissociation
Method
BIAcore T200; blank-surface correction; EPZ6438 comparator
Vehicle
PBS-T with 2% DMSO
Reported limits
SPR replicate count and fit uncertainty not specified in selected methods/caption.
Methods and source locations

Compound reported in the paper: Tanshinone I; Compound label in the paper: Tan I

Evidence concerns the reported research material; Adooq lots were not tested.

Figure 5C-D; Affinity measurement; SI Figure S5A-E

Tan I–zebrafish EZH2 binding: SPR fit; author-reported value, not curve estimation — Figure 5C-D; associated Results

PRC2 methylation assay

Biochemical assay · Wild-type recombinant PRC2 with recombinant H3.3 [1]

Tan I reduced PRC2-mediated H3K27 methylation. H3 and EZH2 loading controls and a no-PRC2 control accompany the blots.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
PRC2-mediated H3K27 methylationQualitative inhibition Reduced at 5 and 10 µM[1]

Literature-Reported Treatment Conditions

Treatment concentration
5 and 10 µM
Exposure duration
30 min preincubation; 60 min methylation reaction
Method
Immunoblot methylation endpoint; SAM present
Vehicle
2% DMSO
Reported limits
No enzymatic IC50 or quantitative replicate count specified in selected assay description.
Methods and source locations

Compound reported in the paper: Tanshinone I; Compound label in the paper: Tan I

Evidence concerns the reported research material; Adooq lots were not tested.

Figure 5E-F; In vitro methyltransferase assay; SI Figure S5F

PRC2-mediated H3K27 methylation: Immunoblot for H3K27me1/me2/me3; H3 and EZH2 controls — Figure 5E-F

Aurora A knockdown and T1 antiproliferative activity

Cell-based study · H1299 human NSCLC cells with control or Aurora A siRNA [2]

Aurora A knockdown reduced baseline proliferation and attenuated the additional response to T1. This supports functional involvement, without establishing direct kinase inhibition.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Proliferation after Aurora A silencing without T1Reduction 45%[2]
Additional T1 antiproliferative response after Aurora A silencingQualitative dependency Attenuated relative to control-siRNA cells[2]

Literature-Reported Treatment Conditions

Treatment concentration
1.0 and 2.0 µM T1; 33 nM siRNA
Exposure duration
72 h drug incubation in shared proliferation method
Method
MTS; control siRNA versus Aurora A siRNA
Vehicle
DMSO drug vehicle
Reported limits
Drug/siRNA timing beyond shared methods is not explicit; vehicle percentage not specified.
Methods and source locations

Compound reported in the paper: Tanshinone I; Compound label in the paper: T1

Evidence concerns the reported research material; Adooq lots were not tested.

Figure 3; Aurora A Silencing by siRNA; Cell Culture and Cell Proliferation Assay; associated Results

Proliferation after Aurora A silencing without T1: MTS; Figure 3 reports mean ± SEM of three independent experiments in triplicate — Figure 3 and associated Results

Additional T1 antiproliferative response after Aurora A silencing: Comparison within Figure 3; no exact values digitized — Figure 3

In Vivo Studies

In a H1299 xenograft prevention model, daily oral tanshinone I begun before implantation reduced final tumor weight by 34.0% at 200 mg/kg body weight (P=0.012). Food intake and body weight were not significantly altered. [2]

H1299 xenograft prevention model

Animal study · Six-week-old female SCID mice; subcutaneous H1299 xenografts [2]

Tumor weight decreased; food intake and body weight were not significantly altered. These limited tolerability readouts do not establish general safety.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Final tumor weight versus vehicleReduction 27.3%[2]
Final tumor weight versus vehicleReduction 34.0%; P=0.012[2]
Food intake and body weightReported comparison No significant alteration[2]

Conditions shared by the study groups

Route
Oral gavage
Frequency
Daily
Treatment course
10-day pretreatment, continued after implantation; methods report 32 days
Vehicle
100 µL corn oil
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
Vehicle control—Reference group[2]
T1 80 mg/kg
80 mg/kg body weight		Corn-oil vehicle groupFinal tumor weight reduced by 27.3%; significance not asserted.[2]
T1 200 mg/kg
200 mg/kg body weight		Corn-oil vehicle groupFinal tumor weight reduced by 34.0%; P=0.012.[2]
Vehicle control
Model: Female SCID mice, H1299 xenograft; n=12/group
Reported limits: Figure 4 timeline spans 6 weeks; exact alignment with methods is not explained.
T1 80 mg/kg
Model: Female SCID mice, H1299 xenograft; n=12/group
Reported limits: Figure 4 timeline spans 6 weeks; exact alignment with methods is not explained.
T1 200 mg/kg
Model: Female SCID mice, H1299 xenograft; n=12/group
Reported limits: Figure 4 timeline spans 6 weeks; exact alignment with methods is not explained.
Methods and source locations

Compound reported in the paper: Tanshinone I; Compound label in the paper: T1

Evidence concerns the reported research material; Adooq lots were not tested.

Figure 4A-D; Animal Study; corresponding Results

Final tumor weight versus vehicle: Excised tumor weight; no significance claim adopted for 80 mg/kg — Figure 4B and associated Results

Final tumor weight versus vehicle: Excised tumor weight; mean ± SEM, n=12/group; Figure 4B marks P<0.05 — Figure 4B and associated Results

Food intake and body weight: Weekly measurements; mean ± SEM, n=12/group — Figure 4C-D; corresponding Results

Vehicle control · Animal Study; Figure 4A-D; corresponding Results

T1 80 mg/kg · Animal Study; Figure 4A-D; corresponding Results

T1 200 mg/kg · Animal Study; Figure 4A-D; corresponding Results

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 568-73-0
Applications Phospholipase inhibitor
Formula C18H12O3
Molecular Weight 276.3
SMILES
CC1=CC=CC2=C1C=CC3=C2C(=O)C(=O)C4=C3OC=C4C

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 21 mg/mL (76 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Huang Y, Yu SH, Zhen WX, et al. Tanshinone I, a new EZH2 inhibitor restricts normal and malignant hematopoiesis through upregulation of MMP9 and ABCG2 Theranostics (2021). PMID: 34093860 DOI: 10.7150/thno.53170 Source material
  2. [2] Li Y, Gong Y, Li L, et al. Bioactive tanshinone I inhibits the growth of lung cancer in part via downregulation of Aurora A function Molecular carcinogenesis (2013). PMID: 22389266 DOI: 10.1002/mc.21888 Source material

Publications

1 publication citing this product

  1. Kumar R, .et al. , Mol Biol Rep, 2018, Oct 11 PMID: 30311125

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