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MedChemExpress - Model WDR5-0103 - ...

MedChemExpress - Model WDR5-0103 - 890190-22-4

FromMedChemExpress LLC (MCE)

WDR5-0103 is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with Kd of 450 nM.

WDR5-0103

MCE China：WDR5-0103

Brand：MedChemExpress (MCE)

Cat. No.HY-19347

CAS：890190-22-4

Synonyms：WD-Repeat Protein 5-0103

Purity：99.93%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：WDR5-0103 (WD-Repeat Protein 5-0103) is a potent and selective WD repeat-containing protein 5 (WDR5) antagonist with a Kd of 450 nM. WDR5-0103 competitively binds to the peptide-binding pocket of WDR5, blocking the interaction between WDR5 and mixed-lineage leukemia (MLL) protein and inhibiting the methyltransferase activity of MLL. WDR5-0103 is mainly used in the research of cancer and neurodegenerative diseases.

In Vitro：WDR5-0103 (5-20 μM; 72 hours) can sensitize ABCB1- or ABCG2-overexpressing multidrug-resistant cancer cells to conventional cytotoxic drugs in a concentration-dependent manner in experiments with multiple cell lines[2]. WDR5-0103 (1-10 μM; 72 hours) does not alter the protein expression of ABCB1 or ABCG2 in multidrug-resistant cancer cells[2]. WDR5-0103 (10 μM; 48 hours) can significantly restore drug-induced apoptosis in ABCB1- or ABCG2-overexpressing multidrug-resistant cancer cells[2].

In Vivo：WDR5-0103 (2.5 mg/kg; intraperitoneal injection; once a day; for 3 days) can reduce the level of H3K4me3, improve cognitive deficits and restore synaptic function in P301S transgenic Tau mice[3]. WDR5-0103 (2.5 mg/kg; intraperitoneal injection; three times) can reduce the level of H3K4me3 in the prefrontal cortex and improve cognitive function in 5xFAD mice[3].

References：

[1]. Senisterra G, et al. Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5. Biochem J. 2013 Jan 1;449(1):151-159. [Content Brief]

[2]. Wu CP, et al. The WD repeat-containing protein 5 (WDR5) antagonist WDR5-0103 restores the efficacy of cytotoxic drugs in multidrug-resistant cancer cells overexpressing ABCB1 or ABCG2. Biomed Pharmacother. 2022 Oct;154:113663. [Content Brief]

[3]. Cao Q, et al. Targeting histone K4 trimethylation for treatment of cognitive and synaptic deficits in mouse models of Alzheimer's disease. Sci Adv. 2020 Dec 9;6(50):eabc8096. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。