Alternate TextTo enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
Home > Molecular Glues

NRX-252114

  Cat. No.:  DC20252   Featured
Chemical Structure
2763260-39-3
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
NRX-252114 is a potent enhancer of the interaction between β-catenin and its cognate E3 ligase, SCFβ-TrCP. It significantly strengthens the binding of the pSer33/S37A β-catenin peptide to β-TrCP, exhibiting an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 also induces the degradation of mutant β-catenin.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2763260-39-3
Chemical Name: NRX-252114
Synonyms: 1H-Isoindole-4-carbonitrile, 2-[[4-[(2,6-dichlorophenyl)thio]-1,2-dihydro-2-oxo-6-(trifluoromethyl)-3-pyridinyl]carbonyl]-2,3-dihydro-;NRX-252114
SMILES: C1C2=C(C(C#N)=CC=C2)CN1C(C1=C(SC2=C(Cl)C=CC=C2Cl)C=C(C(F)(F)F)NC1=O)=O
Formula: C22H12Cl2F3N3O2S
M.Wt: 510.31579208374
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: NRX-252114 is a potent enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-252114 enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP with an EC50 of 6.5 nM and a Kd of 0.4 nM. NRX-252114 induces mutant β-catenin degradation.
Target: EC50: 6.5 nM (β-catenin:β-TrCP Interaction) Kd: 0.4 nM (β-catenin:β-TrCP Interaction)
In Vitro: NRX-252114 (20 μM) enhances the binding of pSer33/S37A β-catenin peptide for β-TrCP, with more than 1500-fold co-operativity. NRX-252114 (0-25 μM) increases the ubiquitylation of pSer33/S37A β-catenin peptide to form long ubiquitin chains. NRX-252114 (0-25 μM) enhances the ubiquitylation of S33E/S37A β-catenin protein, as well as unphosphorylated Ser33/S37A β-catenin peptides. NRX-252114 (20 μM, 6 h) results in robust S33E/S37A β-catenin:β-TrCP interaction in the transfected HEK293T cells.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC60864 D927 (DS11252927) D927 is a molecular glue and promotes glucose uptake in the absence of insulin. D927 also increases the affinity of RAS binding to PI3Kα by ~500-fold. In vivo, D927 mimicks the effects of insulin and rapidly lowers blood glucose concentrations.
DC60863 D223 (DS02312223) D223 is a molecular glue and promotes glucose uptake in the absence of insulin. D223 also increases the affinity of RAS binding to PI3Kα by ~500-fold.
DC60858 LC-04-045 LC-04-045 is a leading NEK7 molecular glue degrader with DC50 of 7 nM and Dmax of 90 % in MOLT-4 cells. LC-04-045 displays high selectivity for NEK7 across the proteome.
DC60852 PVTX-405 PVTX-405 is a potent, effective, highly selective, and orally efficacious IKZF2 molecular glue degrader with DC50 of  0.7 nM. PVTX-405 in combination with anti-PD1 or anti-LAG3 significantly increases animal survival compared to anti-PD1 or anti-LAG3 alone.
DC60837 MGD-28 MGD-28 is a potent molecular glue degrader that demonstrates significant in vitro efficacy against various hematological cancer cell lines. It induces degradation of Ikaros family zinc finger proteins 1, 2, and 3 (IKZF1/2/3) and casein kinase 1 alpha (CK1α) with nanomolar potency via a Cullin-cereblon (CRBN) dependent pathway. Compared to lenalidomide and pomalidomide, MGD-28 achieves deeper, faster, and more potent degradation of these neosubstrates. Additionally, MGD-28 exhibits broad antiproliferative activity in multiple solid malignancies and shows preferential cytotoxicity toward multiple myeloma patient-derived cells at various disease stages.
DC67413 MRT-23227
DC67412 MRT-3486 MRT-3486 (Compound 5) is a cereblon-based NEK7 molecular glue degrader. MRT-3486 can be used for autoinflammatory diseases research.
DC67411 MRT-7612
DC67410 MRT-10350
DC67407 IKZF1-degrader-1 IKZF1-degrader-1 (Compound 9-B) is a highly potent molecular glue that achieves sub-nanomolar degradation of IKZF1 (DC50 = 0.134 nM), demonstrating significant therapeutic potential for targeting IKZF1-dependent malignancies.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia