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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
9 Results for "
Y220C mutation
" in MedChemExpress (MCE) Product Catalog:
Products (9)
9 Results for "Y220C mutation" in MCE Product Catalog:
3
Rezatapopt (PC14586) is an orally active antineoplastic agent. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure. Rezatapopt demonstrates tumor inhibition and regression in mouse models with established human tumor xenografts harboring the TP53 Y220C mutation .
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1 Cited Publications
p53 Activator 7 is a p53 mutation Y220C (MDM-2/p53) activator with an EC50 of 104 nM. p53 Activator 7 can bind to p53 mutant and restore its ability to bind DNA (WO2022213975A1; Example B-1) . p53 Activator 7 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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1 Cited Publications
MB710, an aminobenzothiazole derivative, is a stabilizer of oncogenic p53 mutation Y220C. MB710 binds tightly to the Y220C pocket and stabilizes p53-Y220C, with a Kd of 4.1 μM. MB710 shows anticancer activity in p53-Y220C cell lines .
Cat. No.: HY-179560
Research Areas:
PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53 Y220C-PLK1 ternary complex (EC50 = 1.4 μM). PMV6-PEG4-BI2536 causes PLK1 mislocalization and inhibits PLK1 activity, inducing G2/M phase arrest and apoptosis in p53 Y220C-mutant cells, while sparing cells with wild-type TP53. PMV6-PEG4-BI2536 can be used in research on uterine, gastric, pancreatic, prostate, and breast cancers harboring the p53 Y220C mutation. PMV6-PEG4-BI2536 is composed of PMV6 (a p53 Y220C mutant-binding ligand), PEG4 (a linker), and BI2536 (HY-159493) (a PLK inhibitor) .
Cat. No.: HY-W287494
CAS No.: 38470-63-2
Antitumor agent-202 is a stabilizer of the p53 Y220C mutant. It exhibits a selective inhibitory effect on the proliferation of tumor cells carrying the p53 Y220C mutation and can be applied to the research of cancers associated with the p53 Y220C mutation .
Cat. No.: HY-184397
P53-Y220C stabilizer-1 as an indole-based p53-Y220C stabilizer (EC50 = 0.46 μM) that engages the mutation-induced cavity. P53-Y220C stabilizer-1 binds the p53-Y220C mutant with high affinity (KD = 56 nM) and acts as a selective indole-based p53-Y220C stabilizer that engages the mutation-induced cavity. P53-Y220C stabilizer-1 increases mutant protein thermal stability and restores p53 transcriptional activity, mainly triggering cell cycle arrest instead of acute apoptosis. P53-Y220C stabilizer-1 can be applied to cancers harboring the p53-Y220C mutation, such as gastric cancer .
Cat. No.: HY-184518
Target:
Research Areas:
P53/BET TCIP-1 (Compound 47) is a dual-functional hybrid molecule that possesses both reactivation of p53 Y220C (EC50 ≤ 100 nM) and inhibition of BRD4/BET (EC50 ≤ 500 nM) dual activities. P53/BET TCIP-1 exhibits significant inhibitory proliferation activity in p53 Y220C mutant tumor cells. P53/BET TCIP-1 can be used to study p53 Y220C mutation-related cancers (such as ovarian cancer, pancreatic cancer, gastric cancer, etc.) .
Cat. No.: HY-164828
CAS No.: 2636846-37-0
Synonyms: PC14586 analog-1
Rezatapopt analog-1 (PC14586 analog-1) (1919) is a Rezatapopt (HY-156633) analog. Rezatapopt binds to a pocket created by the TP53 Y220C mutation. Rezatapopt restores p53 tumor suppressor functions by stabilization of the p53 protein structure .
Cat. No.: HY-186101
CAS No.: 3107623-69-5
P53 mutant stabilizer-1 (compound 274) is a covalent mutant p53 stabilizer. P53 mutant stabilizer-1 can be used for the study of wild-type function of p53 mutants, such as cancers associated with p53 mutation .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
