GNE-1567
GNE-1567 is a potent ERα PROTAC degrader and a XIAP antagonist with a Kd of 0.03 μM. GNE-1567 induces ubiquitination and degradation of ERα by recruiting the E3 ubiquitin ligase XIAP, thereby achieving the dual effects of ERα protein elimination and abrogation of XIAP-mediated apoptosis inhibition simultaneously. GNE-1567 can be used in studies related to ERα-dependent breast cancer.
(Pink: ERα ligand (HY-18719); Blue: XIAP ligand (HY-175449); Black: linker).
For research use only. We do not sell to patients.
- Formula: C60H65BrN6O9
- Molecular Weight:1094.10
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
XIAP 0.03 μM (Kd) |
In Vitro
GNE-1567 (1 nM-1 μM; 4-144 h) dose-dependently degrades ERα protein in MCF-7 cells; it slightly inhibits cell proliferation, but does not induce obvious cell death or activation of Caspase-3/7; it does not cause processing of p100 to p52 or induce TNFα expression.
GNE-1567 (250 nM; 24 h-72 h) does not significantly upregulate the expression of cellular immune factors in MCF-7, EFM-19 and PBMCs[1].
GNE-1567 (1 nM-1 μM; 4-144 h) induces dose-dependent degradation of ERα and moderately inhibits cell proliferation in EFM19, CAMA-1, T47D, HCC1428, BT474M1, and MDA-MB-134VI cells[1].
The degradation of ERα induced by GNE-1567 (100-250 nM; 4 h) in MCF-7 cells is blocked by XIAP siRNA knockdown, Bortezomib (HY-10227) and MLN7243 (HY-100487), but is not affected by the NAE1 inhibitor MLN4924 (HY-70062).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MCF-7, EFM19, CAMA-1, T47D, HCC1428, BT474M1, MDA-MB-134VI
-
Concentration:1, 10, 100, 1000 nM
-
Incubation Time:4 h
-
Result:Significantly degraded the ERα protein in the aforementioned ERα-positive breast cancer cell lines, but did not degrade XIAP or cIAP1 proteins.
-
Cell Line:MCF-7
-
Concentration:250 nM
-
Incubation Time:24 h, 48 h, 72 h
-
Result:Did not significantly upregulate the mRNA expression of TNFα.
-
Cell Line:MCF-7
-
Concentration:250 nM
-
Incubation Time:24 h, 48 h, 72 h
-
Result:Did not promote the processing of p100 to p52.
Chemical Information
-
Molecular Weight 1094.10
-
Formula C60H65BrN6O9
-
SMILES
CC/C(C1=CC=CC=C1)=C(C2=CC=C(O)C=C2)/C3=CC=C(C=C3)OCCN(C(CCOCCOCCC(N4C5=C(N(C([C@H]([C@@H]4C)NC([C@@H](NC)C)=O)=O)CC6=C(C=CC7=C6C=CC(Br)=C7)OC)C=CC(C#N)=C5)=O)=O)C
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GNE-1567 Related Classifications
HY-175448 Related Classifications
Powered by Bioz