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Cat. No.: HY-155490

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Nur77 antagonist 1

Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(K_D^SPR_Nur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells.

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

CAS No.: 2378780-25-5
Formula: C₂₅H₃₂N₈OS
Molecular Weight:492.64

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

Nur77 antagonist 1 Chemical Structure

CAS No.: 2378780-25-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Nur77/NR4A1

All Nuclear Hormone Receptor 4A/NR4A Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Bel-7402	IC₅₀	38.33 μM Compound: ja	Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human Bel-7402 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
BT-549	IC₅₀	2.12 μM Compound: ja	Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human BT-549 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
HCC1806	IC₅₀	0.38 μM Compound: ja	Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
HCT-116	IC₅₀	9.84 μM Compound: ja	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
HeLa	IC₅₀	1.99 μM Compound: ja	Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
HeLa	IC₅₀	9.15 μM Compound: ja	Antiproliferative activity against human HeLa cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
HepG2	IC₅₀	53.72 μM Compound: ja	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
HT-29	IC₅₀	47.16 μM Compound: ja	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
MCF-10A	IC₅₀	48.01 μM Compound: ja	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
MCF7	IC₅₀	0.72 μM Compound: ja	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
MDA-MB-231	IC₅₀	0.4 μM Compound: ja	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
SW-620	IC₅₀	18.09 μM Compound: ja	Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human SW620 cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
T47D	IC₅₀	1.05 μM Compound: ja	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]
T47D	IC₅₀	6.34 μM Compound: ja	Antiproliferative activity against human T47D cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay Antiproliferative activity against human T47D cells transfected with Nur77 siRNA assessed as inhibition of cell growth measured after 24 hrs by MTT assay	[PMID: 37983615]

In Vitro

Nur77 antagonist 1(Compound ja), shows selectivity against tumor cells from different tissues, possesses highly selective antiproliferative activity toward all tested TNBC cell lines (IC₅₀: 0.40 ± 0.03, 0.38 ± 0.08, 2.12 ± 0.15 for MDA-MB-231,HCC-1806, and BT549) compared to the human normal breast cell line (IC₅₀: 48.01 ± 2.86 for MCF-10A)^[1].
Nur77 antagonist 1 (0-2 μM, 6 h) induces MDA-MB-231-sictr cells apoptosis in a Nur77-dependent manner^[1].
Nur77 antagonist 1 (0-5 μM, 6 h) induces Nur77-dependent cell-cycle arrest and apoptosis by mediating the TP53 phosphorylation pathway in MDA-MB-231 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

0-5 μM
Incubation Time:

6 h
Result:

Induced extrinsic Nur77 degradation.
Induced PARP cleavage in a dose- and time-dependent manner in MDA-MB-231 cells.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

0.32-5 μM
Incubation Time:

5 h
Result:

Exhibited the apoptotic cells accounted for 15.10, 25.38, 40.01, 54.83, and 74.62% at 0.32, 0.63, 1.25, 2.5, and 5.0 μM.

In Vivo

Nur77 antagonist 1(Compound ja) (10 mg/kg, i.p) has excellent antitumor efficiency and good in vivo tolerance in the breast cancer MDA-MB-231 xenograft nude mice model^[1].
Nur77 antagonist 1 (1.25-5 μM) has good in vivo safety in zebrafish embryo model^[1].

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

Animal Model:

the breast cancer MDA-MB-231 xenograft nude mice model^[1]
Dosage:

10 mg/kg
Administration:

i.p
Result:

Reduced tumor weight and volume with tumor growth inhibition (TGI) of 99.95%.
Increased cleaved caspase 3 and decreased the proliferation marker Ki67 expression in tumor tissues.

Chemical Information

CAS No. 2378780-25-5
Molecular Weight 492.64
Formula C₂₅H₃₂N₈OS
SMILES

CCN(CC)CCCNC(C1=CC2=C(N1)C=CC(NC3=NC=CC(C4=C(N=C(S4)NC)C)=N3)=C2)=O
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Qin J, et al. Discovery of 5-(Pyrimidin-2-ylamino)-1H-indole-2-carboxamide Derivatives as Nur77 Modulators with Selective and Potent Activity Against Triple-Negative Breast Cancer. J Med Chem. 2023 Nov 20. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Nur77 antagonist 1

All Nuclear Hormone Receptor 4A/NR4A Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Nur77 antagonist 1 Related Classifications

HY-155490 Related Classifications