Grouped product items

SKU

Size

Availability

Price

Qty

M125960-10mg

10mg

In stock

$14.90

M125960-25mg

25mg

In stock

$29.90

M125960-50mg

50mg

Available within 4-8 weeks(?)

$47.90

M125960-100mg

100mg

Available within 8-12 weeks(?)

$85.90

Basic Description

Synonyms	2-Methoxyestradiol\|362-07-2\|Panzem\|2-Methoxyestradiol-17beta\|2-ME2\|2-Hydroxyestradol 2-methyl ether\|2ME2\|2-MeOE2\|Estradiol, 2-methoxy-\|2-Methoxyestradiol (2-MeOE2)\|NSC-659853\|2-methoxyoestradiol\|2-Hydroxyestradiol 2-methyl ether\|2-methoxy-17beta-estradiol
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	2-methoxyestradiol (2ME2) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 ± 0.11 μM for the inhibition of BPAEC migration.2-Methoxyestradiol is an endogenous estrogen metabolite with low affinity for
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	AGONIST
Mechanism of action	Agonist of GPER
Note	Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description	2-Methoxyestradiol (2-MeOE2) depolymerizes microtubules and blocks HIF-1α nuclear accumulation and HIF-transcriptional activity. Phase 2. A disruptor of microtubule function and HIF-1 inhibitor

Associated Targets

CYP1B1 Tchem Cytochrome P450 1B1 0 Activities

Discover Target: CYP1B1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR1 Tclin Estrogen receptor 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EHMT2 Tchem Histone-lysine N-methyltransferase EHMT2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR2 Tclin Estrogen receptor beta 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CBX1 Tbio Chromobox protein homolog 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GMNN Tbio Geminin 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC22A1 Tchem Solute carrier family 22 member 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KMT2A Tchem Histone-lysine N-methyltransferase 2A 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HDAC6 Tclin Histone deacetylase 6 0 Activities

Discover Target: HDAC6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TXNRD1 Tclin Thioredoxin reductase 1, cytoplasmic 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TUBB2B Tclin Tubulin beta-2B chain 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

UGT2B7 Tchem UDP-glucuronosyltransferase 2B7 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TUBA1A Tchem Tubulin alpha-1A chain 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SHBG Tchem Sex hormone-binding globulin 1 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PMP22 Tbio Peripheral myelin protein 22 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RGS4 Tchem Regulator of G-protein signaling 4 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

LMNA Tbio Prelamin-A/C 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GAA Tclin Lysosomal alpha-glucosidase 0 Activities

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MPHOSPH8 Tbio M-phase phosphoprotein 8 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP19A1 Tclin Aromatase 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP1A1 Tchem Cytochrome P450 1A1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BLM Tchem Bloom syndrome protein 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ATXN2 Tbio Ataxin-2 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

APOBEC3G Tchem DNA dC->dU-editing enzyme APOBEC-3G 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TARDBP Tchem TAR DNA-binding protein 43 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPT Tclin Microtubule-associated protein tau 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ATAD5 Tbio ATPase family AAA domain-containing protein 5 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPER1 Tchem G-protein coupled estrogen receptor 1 0 Activities

Discover Target: GPER1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GLP1R Tclin Glucagon-like peptide 1 receptor 0 Activities

Discover Target: GLP1R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

IDH1 Tclin Isocitrate dehydrogenase [NADP] cytoplasmic 0 Activities

Discover Target: IDH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NFE2L2 Tchem Nuclear factor erythroid 2-related factor 2 0 Activities

Discover Target: NFE2L2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MTOR Tclin Serine/threonine-protein kinase mTOR 0 Activities

Discover Target: MTOR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	(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	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
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
WGK Germany	3
RTECS	KG7537500
PubChem CID	66414
Molecular Weight	302.41

Database links

PubChem CID	66414
CAS Registry No.	362-07-2
ChEMBL Ligand	CHEMBL299613
BindingDB Ligand	50060957
DrugBank Ligand	DB02342
RCSB PDB Ligand	ESM, ESM

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

17 results found

Lot Number	Certificate Type	Date	Item
K2209723	Certificate of Analysis	Aug 15, 2024	M125960
K2209699	Certificate of Analysis	Aug 15, 2024	M125960
G2411668	Certificate of Analysis	May 20, 2024	M125960
G2411666	Certificate of Analysis	May 20, 2024	M125960
G2411664	Certificate of Analysis	May 20, 2024	M125960
G2411662	Certificate of Analysis	May 20, 2024	M125960
B2421544	Certificate of Analysis	Jan 31, 2024	M125960
B2421556	Certificate of Analysis	Jan 31, 2024	M125960
B2421547	Certificate of Analysis	Jan 31, 2024	M125960
B2421546	Certificate of Analysis	Jan 31, 2024	M125960
B2421545	Certificate of Analysis	Jan 31, 2024	M125960
B2421543	Certificate of Analysis	Jan 31, 2024	M125960
H2329099	Certificate of Analysis	Oct 27, 2022	M125960
I2307032	Certificate of Analysis	Oct 27, 2022	M125960
K2209721	Certificate of Analysis	Oct 27, 2022	M125960
K2209722	Certificate of Analysis	Oct 27, 2022	M125960
K2209731	Certificate of Analysis	Oct 27, 2022	M125960

Chemical and Physical Properties

Solubility	Soluble in DMSO (10 mg/mL), ethanol (10 mg/mL), chloroform, ethanol (1 mg/ml), and 1:1DMF:PBS(pH7.2) (0.5 mg/ml). Insoluble in water.
Specific Rotation[α]	107° (C=0.5,THF)
Melt Point(°C)	187 °C

Safety and Hazards(GHS)

Pictogram(s)	GHS06, GHS08, GHS09, GHS07
Signal	Danger
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H301:Toxic if swallowed H311:Toxic in contact with skin H331:Toxic if inhaled H400:Very toxic to aquatic life H410:Very toxic to aquatic life with long lasting effects H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child H350:May cause cancer H301+H311+H331:Toxic if swallowed, in contact with skin or if inhaled
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P271:Use only outdoors or in a well-ventilated area. P270:Do not eat, drink or smoke when using this product. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P391:Collect spillage. P330:Rinse mouth. P361+P364:Take off immediately all contaminated clothing and wash it before reuse. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P316:IF SWALLOWED: Get emergency medical help immediately. P318:if exposed or concerned, get medical advice. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P316:Get emergency medical help immediately. P319:Get medical help if you feel unwell.
WGK Germany	3
RTECS	KG7537500

Alternative Products

References

1. Pribluda VS, Gubish Jr ER, Lavallee TM, Treston A, Swartz GM, Green SJ. (2000) 2-Methoxyestradiol: an endogenous antiangiogenic and antiproliferative drug candidate.. Cancer Metastasis Rev, 19 (1-2): (173-9). [PMID:11191057]
2. Lakhani NJ, Sarkar MA, Venitz J, Figg WD. (2003) 2-Methoxyestradiol, a promising anticancer agent.. Pharmacotherapy, 23 (2): (165-72). [PMID:12587805]
3. Sidor C, D'Amato R, Miller KD. (2005) The potential and suitability of 2-methoxyestradiol in cancer therapy.. Clin Cancer Res, 11 (16): (6094-5). [PMID:16115955]
4. Dahut WL, Lakhani NJ, Gulley JL, Arlen PM, Kohn EC, Kotz H, McNally D, Parr A, Nguyen D, Yang SX et al.. (2006) Phase I clinical trial of oral 2-methoxyestradiol, an antiangiogenic and apoptotic agent, in patients with solid tumors.. Cancer Biol Ther, 5 (1): (22-7). [PMID:16357512]
5. Koganti S, Snyder R, Thekkumkara T. (2012) Pharmacologic effects of 2-methoxyestradiol on angiotensin type 1 receptor down-regulation in rat liver epithelial and aortic smooth muscle cells.. Gend Med, 9 (2): (76-93). [PMID:22366193]
6. Thekkumkara T, Snyder R, Karamyan VT. (2016) Competitive Binding Assay for the G-Protein-Coupled Receptor 30 (GPR30) or G-Protein-Coupled Estrogen Receptor (GPER).. Methods Mol Biol, 1366 (3): (11-17). [PMID:26585123]
7. Prossnitz ER, Arterburn JB. (2015) International Union of Basic and Clinical Pharmacology. XCVII. G Protein-Coupled Estrogen Receptor and Its Pharmacologic Modulators.. Pharmacol Rev, 67 (3): (505-40). [PMID:26023144]
8. Liu J et al.. (2019) CCR7 Chemokine Receptor-Inducible lnc-Dpf3 Restrains Dendritic Cell Migration by Inhibiting HIF-1a-Mediated Glycolysis.. Immunity, 50 (3): (600-615.e15). [PMID:30824325]

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2-Methoxyestradiol (2-MeOE2) - ≥98%, high purity , CAS No.362-07-2, Agonist of GPER