Table of Contents
2-Methoxyestradiol 0.55μM R07 exp310
Mechanism of Action
Endogenous estradiol metabolite, weak agonist for estrogen receptor, agonist of GPER1, microtubule destabilizer
- Class / Subclass 1: Metabolism / Metabolite
- Class / Subclass 2: Signal Transduction / GPCR Agonist
- Class / Subclass 3: Cell Cycle / Microtubule Poison
Technical Notes
Protein References
- PubChem Name: 2-Methoxyestradiol
- Synonyms: 2-ME2; NSC-659853
- CAS #: 362-07-2
- PubChem CID: 66414
- IUPAC: (8R,9S,13S,14S,17S)-2-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
- INCHI Name: InChI=1S/C19H26O3/c1-19-8-7-12-13(15(19)5-6-18(19)21)4-3-11-9-16(20)17(22-2)10-14(11)12/h9-10,12-13,15,18,20-21H,3-8H2,1-2H3/t12-,13+,15-,18-,19-/m0/s1
- INCHI Key: CQOQDQWUFQDJMK-SSTWWWIQSA-N
- Molecular Weight: 302.4
- Canonical SMILES: CC12CCC3C(C1CCC2O)CCC4=CC(=C(C=C34)OC)O
- Isomeric SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)CCC4=CC(=C(C=C34)OC)O
- Molecular Formula: C19H26O3
Protein Supplier
- Supplier Name: Toronto Research Chemicals
- Catalog #: M262625
- Lot #: 1-GNM-86-4
Protein Characterization
- HRMS (ESI-TOF) m/z: (M+H)+ Calcd for C19H26O3 303.19547; found 303.19491
Dose Response Curve
- Platform ID: Methoxy_b-Estradiol
- Min: -4.8666; Max: 98.0088
| IC | Concentration (µM) |
|---|---|
| IC10 | N/A |
| IC20 | 0.1847 |
| IC30 | 0.2756 |
| IC40 | 0.3897 |
| IC50 | 0.5415 |
| IC60 | N/A |
| IC70 | N/A |
| IC80 | N/A |
| IC90 | N/A |
Screen Summary
- Round: 07
- Dose: 550nM
- Days of incubation: 8
- Doublings: 6.5
- Numbers of reads: 24035096
Screen Results
| Sensitive/Resistant hits (FDR<0.05) | CRANKS | Score Plot | Top 30 Genes | Screen Similarity | Top 30 Sensitive GO terms | Top 30 Resistant GO terms |
|---|---|---|---|---|---|---|
| 4/0 | Scores |
2-Methoxyestradiol 0.55μM R07 exp310
2-Methoxyestradiol 0.55μM R07 exp310 vs UMK57 0.6μM R03 exp107
2-Methoxyestradiol 0.55μM R07 exp310 vs S-trityl-L-cysteine 0.5μM R05 exp243
2-Methoxyestradiol 0.55μM R07 exp310 vs BML-284 0.09μM R08 exp460
2-Methoxyestradiol 0.55μM R07 exp310 vs Vincristine 0.0005μM R04 exp190
2-Methoxyestradiol 0.55μM R07 exp310 vs Combretastatin A4 0.002 to 0.003μM day4 R04 exp179
2-Methoxyestradiol 0.55μM R07 exp310 vs Mdivi-1 15μM R05 exp217
2-Methoxyestradiol 0.55μM R07 exp310 vs UMK57 1μM R01 exp59
2-Methoxyestradiol 0.55μM R07 exp310 vs Ixabepilone 0.004 to 0.005μM on day4 R04 exp184
2-Methoxyestradiol 0.55μM R07 exp310 vs Quercetin 20μM R08 exp517
2-Methoxyestradiol 0.55μM R07 exp310 vs Demecolcine 0.03μM R05 exp228
2-Methoxyestradiol 0.55μM R07 exp310 vs Cabazitaxel 0.001μM R05 exp223
2-Methoxyestradiol 0.55μM R07 exp310 vs Vinblastine 0.002μM R01 exp60
2-Methoxyestradiol 0.55μM R07 exp310 vs Docosahexaenoic-acid 50μM R07 exp356
2-Methoxyestradiol 0.55μM R07 exp310 vs HMS-I1 1μM R01 exp46
2-Methoxyestradiol 0.55μM R07 exp310 vs Rifampicin 10μM R00 exp32
2-Methoxyestradiol 0.55μM R07 exp310 vs Colchicine 0.009μM R05 exp215
2-Methoxyestradiol 0.55 to 0.75μM on day4 R07 exp311 vs 2-Methoxyestradiol 0.55μM R07 exp310
2-Methoxyestradiol 0.55 to 1μM on day4 R07 exp312 vs 2-Methoxyestradiol 0.55μM R07 exp310
