2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
  3. RAR/RXR
  4. ER 50891

ER 50891 is a RARα antagonist. ER 50891 can significantly antagonize the inhibitory effect of all-trans retinoic acid (ATRA) on the total cell metabolic activity and proliferation of MC3T3-E1 preosteoblasts. ER 50891 rescues ATRA-inhibited osteocalcin (OCN) expression and extracellular matrix mineralization, and suppresses alkaline phosphatase (ALP) activity synergistically. ER 50891 can be used for the study of osteoporosis related to ATRA-induced inhibition of osteoblastogenesis.

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

ER 50891

ER 50891 Chemical Structure

CAS No. : 187400-85-7

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Based on 1 publication(s) in Google Scholar

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Description

ER 50891 is a RARα antagonist. ER 50891 can significantly antagonize the inhibitory effect of all-trans retinoic acid (ATRA) on the total cell metabolic activity and proliferation of MC3T3-E1 preosteoblasts. ER 50891 rescues ATRA-inhibited osteocalcin (OCN) expression and extracellular matrix mineralization, and suppresses alkaline phosphatase (ALP) activity synergistically. ER 50891 can be used for the study of osteoporosis related to ATRA-induced inhibition of osteoblastogenesis[1].

IC50 & Target[1]

RXR α

 

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
6.4 nM
Compound: 12f
Antagonistic activity was evaluated in terms of inhibition of HL-60 cell differentiation activity by ATRA (10 nM)
Antagonistic activity was evaluated in terms of inhibition of HL-60 cell differentiation activity by ATRA (10 nM)
[PMID: 11354380]
In Vitro

ER 50891 (1-3 μM, 3 days) significantly promotes total cell metabolic activity of MC3T3-E1 preosteoblasts alone and antagonizes the inhibitory effect of ATRA on total cell metabolic activity[1].
ER 50891 (0.25-3 μM, 3 days) dose-dependently relieves the inhibition of 1 μM ATRA on OCN expression in MC3T3-E1 preosteoblasts[1].
ER 50891 (1.5-3 μM, 19 days) rescues the extracellular matrix mineralization of MC3T3-E1 preosteoblasts inhibited by ATRA[1].

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

ER 50891 Related Antibodies
Molecular Weight

432.51

Formula

C29H24N2O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(O)C1=CC=C(C2=CC=C(C3=NC4=C(C(C)C)C=CC=C4C(C5=CC=CC=C5)=C3)N2)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation
References
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ER 50891 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:

ER 50891187400-85-7ER50891ER-50891RAR/RXRRetinoic acid receptorsRetinoid X receptorsall-trans retinoic acidosteocalcinalkaline phosphataseosteoblastogenesisInhibitorinhibitorinhibit

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