2. Vitamin D Related/Nuclear Receptor Immunology/Inflammation
  3. Estrogen Receptor/ERR COX
  4. 4H-Chromen-4-one-o-carborane

4H-Chromen-4-one-o-carborane is an estrogen receptor (ER) agonist, with an EC50 of 0.9 μM for ERα and an EC50 of 11.1 μM for ERβ. 4H-Chromen-4-one-o-carborane also acts as an inhibitor of COX-1 and COX-2, with an IC50 of 6.6 μM for COX-1 and an IC50 of 17.7 μM for COX-2.

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

4H-Chromen-4-one-o-carborane

4H-Chromen-4-one-o-carborane Chemical Structure

CAS No. : 3097646-96-0

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4H-Chromen-4-one-o-carborane Related Antibodies

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Description

4H-Chromen-4-one-o-carborane is an estrogen receptor (ER) agonist, with an EC50 of 0.9 μM for ERα and an EC50 of 11.1 μM for ERβ. 4H-Chromen-4-one-o-carborane also acts as an inhibitor of COX-1 and COX-2, with an IC50 of 6.6 μM for COX-1 and an IC50 of 17.7 μM for COX-2[1].

In Vitro

4H-Chromen-4-one-o-carborane (compound 1) (up to 100 μM; 48 h) exhibits only weak antiproliferative activity in HepG2 hepatocellular carcinoma cells (IC50 = 69.5 μM), and shows no activity even at the maximum concentration of 100 μM in Raji, Ramos or PC3 cancer cell lines[1].

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

4H-Chromen-4-one-o-carborane Related Antibodies

Cell Viability Assay[1]

Cell Line: Raji (lymphoma), Ramos (lymphoma), PC3 (prostate cancer), HepG2 (hepatocellular carcinoma)
Concentration: up to 100 μM
Incubation Time: 48 h
Result: Showed negligible antiproliferative activity in Raji, Ramos, and PC3 cell lines, with IC50 values greater than 100 μM for each.
Exhibited weak antiproliferative activity in HepG2 cells, with an IC50 of 69.5 μM.
In Vivo

4H-Chromen-4-one-o-carborane (0.5 mg; i.p.; single dose) has a long blood half-life and slow biodistribution rate. At 3 h after a single i.p. injection, the highest boron uptake occurs in the liver (14.1 μg/g) and blood (11.5 μg/g)[1].

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

Animal Model: athymic mice (male, nu/nu homozygous, 4−6 weeks old)[1]
Dosage: 0.5 mg
Administration: i.p.; single dose
Result: Measured boron content as 11.5 μg/g in blood.
Measured boron content as 14.1 μg/g in liver.
Showed lower boron uptake in all other tested organs (brain, bone, heart, kidney, large intestine, lung, muscle, pancreas, small intestine, spleen, stomach, tumor) than blood.
Molecular Weight

288.35

Formula

C11H16B10O2
CAS No.
SMILES

O=C1C=2C=CC=CC2OC=C1C3456[BH]789[BH]%10%11%12[BH]%13%14%15[BH]%10%169[BH]%13%17%18[BH]%14%19%20[BH]%15%11%21[BH]%1276[BH]%21%195[CH]%17%204[BH]%16%1883
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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4H-Chromen-4-one-o-carborane Related Classifications

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Help & FAQs
  • 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.

Keywords:

4H-Chromen-4-one-o-carborane3097646-96-0Estrogen Receptor/ERRCOXCyclooxygenaseRamoshuman ERαhuman COX-1human ERβHepG2 hepatocellular carcinoma cellshuman COX-2ERβestrogen receptor αPC3RajiInhibitorinhibitorinhibit

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