2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. ERRγ-IN-1

ERRγ-IN-1 is a ERRγ inhibitor with an IC50 of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma.

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ERRγ-IN-1

ERRγ-IN-1 Chemical Structure

CAS No. : 2170732-60-0

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ERRγ-IN-1 Related Antibodies

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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Description

ERRγ-IN-1 is a ERRγ inhibitor with an IC50 of 0.040 μM. ERRγ-IN-1 activates MAPK (p44/p42) and inhibits the activity of ERRγ. ERRγ-IN-1 significantly increases iodine uptake in anaplastic thyroid carcinoma xenografts and suppresses tumor growth in nude mice. ERRγ-IN-1 is applicable for the research of anaplastic thyroid carcinoma[1].

IC50 & Target

ERRγ

0.04 μM (IC50)

ERRβ

1.33 μM (IC50)

ERα

1.24 μM (IC50)

In Vitro

ERRγ-IN-1 (Compound 18a) is a highly potent inverse agonist of ERRγ, with an IC50 of 0.040 μM for binding to ERRγ. It shows extremely weak cross-reactivity with ERRα (IC50 > 10 μM), moderate activity against ERRβ (IC50 = 1.33 μM), and weak binding ability to ERα (IC50 = 1.24 μM), indicating its targeting selectivity for ERRγ[1].
ERRγ-IN-1 (6-12 μM) reduces the ERRγ mRNA expression level by approximately 90% and increases the NIS mRNA expression level by about 2-fold in CAL-62 anaplastic thyroid cancer cells, and this effect depends on the activation of MAPK (p44/p42)[1].
ERRγ-IN-1 (6-12 μM) reduces ERRγ protein levels in a dose-dependent manner and promotes membrane localization of fully glycosylated NIS (the 98 kDa isoform) in CAL-62 ATC cells, a process dependent on the activation of MAPK (p44/p42)[1].
ERRγ-IN-1 (6-12 μM) increases iodine uptake in CAL-62 anaplastic thyroid cancer cells by approximately 2-fold at 12 μM and 1.5-fold at 6 μM (measured as CPM/μg protein), and this effect depends on the activation of MAPK (p44/p42)[1].
Combination of ERRγ-IN-1 and 131I reduces the colony-forming ability of CAL-62 cells by approximately 40%[1].
ERRγ-IN-1 (10 μM) moderately inhibits CYP2D6 (63.5% of the control group) and CYP3A4 (66.4% of the control group), while exerts weak inhibitory effects on CYP1A2 (88% of the control group), CYP2C9 (86.1% of the control group) and CYP2C19 (81.2% of the control group)[1].

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

ERRγ-IN-1 Related Antibodies
In Vivo

ERRγ-IN-1 (100-200 mg/kg; p.o.; daily; 6 days) significantly increases iodine uptake in CAL62 anaplastic thyroid cancer xenografts and inhibits tumor growth in nude mice, with 200 mg/kg showing greater efficacy[1].

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

Animal Model: Balb/c nu/nu (female, 6 weeks old, 18-20 g, implanted with CAL62/effluc tumor cells via trochar)[1]
Dosage: 100 mg/kg; 200 mg/kg
Administration: p.o.; daily; 6 days
Result: Increased tumor iodine uptake to ~0.5 %ID/g at 100 mg/kg; increased tumor iodine uptake to ~1.8 %ID/g at 200 mg/kg.
Reduced bioluminescent tumor signal increase to a mean of ~80 relative units at 100 mg/kg on Day 6 post-treatment.
Reduced bioluminescent tumor signal increase to a mean of ~30 relative units at 200 mg/kg on Day 6 post-treatment.
Caused no significant body weight loss over the 6-day treatment period.
Molecular Weight

456.62

Formula

C30H36N2O2
CAS No.
SMILES

OCCC/C(C1=CC=CC=C1)=C(C2=CC=C(C=C2)O)/C3=CC=C(N4CCN(CC4)C(C)C)C=C3
Shipping

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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ERRγ-IN-1 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:

ERRγ-IN-12170732-60-0Estrogen Receptor/ERRERRγ inhibitoranaplastic thyroid carcinomaBalb/c nu/nu miceInhibitorinhibitorinhibit

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