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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
25 Results for "
Y220C
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "Y220C" in MCE Product Catalog:
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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
PhiKan 083 is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM. PhiKan 083 can be used for cancer research .
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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 .
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1 Cited Publications
PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM , and a relative binding affinity (Kd) of 150 μM in Ln229 cells .
Cat. No.: HY-169369
CAS No.: 3109600-48-5
Synonyms: XJZ-06-462
TRAP-1 (XJZ-06-462) is a transcriptional activator of p53 (TRAP) with JQ-1 carboxylic acid (HY-78695) as its target protein ligand. TRAP-1 forms a ternary complex with p53 Y220C and BRD4, potently activates p53 transcription, and inhibits the growth and proliferation of tumor cells. TRAP-1 upregulates p21 and other p53 target genes in pancreatic cell lines carrying p53 Y220C, and induces cellular senescence and apoptosis. TRAP-1 can be used in cancer research involving p53 Y220C-carrying tumors .
SLMP53-2 is a mutant p53 reactivator. SLMP53-2 restores wild-type-like conformation and DNA-binding ability of mutp53-Y220C by enhancing its interaction with the Hsp70, leading to the reestablishment of p53 transcriptional activity. SLMP53-2 can induce cell cycle arrest, apoptosis and endoplasmic reticulum (ER) stress. SLMP53-2 exhibits antitumor activity .
Cat. No.: HY-160449
CAS No.: 2849484-29-1
p53 Activator 10 (Example C-2) is a compound that targets the y220c mutant of p53. p53 Activator 10 activation is involved in the downstream effects of tumor suppression .
Cat. No.: HY-175318S
CAS No.: 3069395-29-2
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-181616
CAS No.: 3114732-99-6
Target:
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p53-Y220C/PLK1 modulator-1 (compound15) is a dual modulator targeting p53-Y220C and PLK1. p53-Y220C/PLK1 modulator-1 can be used in the cancer .
Cat. No.: HY-160450
CAS No.: 2850211-42-4
p53 Activator 11 (compound A-1) is a potent p53 activator with an EC50 value of 0.478 µM for p53 (Y220C). p53 Activator 11 has the potential for the research of cancer .
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-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-100601
CAS No.: 1446352-68-6
Target:
PK7242 is an inducer of reactivation of mutant p53 in cancer cells. In cancer cells carrying the Y220C mutant, PK7242 binds to the p53-Y220C core domain and induces growth inhibition, cell-cycle arrest, and apoptosis.
Cat. No.: HY-182744
LLQ-45 is a covalent p53 Y220C mutant protein agonist with an EC50 of 24.97 μM. LLQ-45 activates the anti-tumor function of p53 Y220C through covalent modification, restores its DNA-binding ability and enhances its thermal stability. LLQ-45 selectively inhibits the proliferation of p53 Y220C mutant tumor cells, suppresses cell growth and upregulates the expression of CDKN1A. LLQ-45 can be used in studies related to p53 Y220C mutant cancers .
Cat. No.: HY-179507
p53 Activator 17 is a p53-Y220C activator. p53 Activator 17 exhibits selective cytotoxicity and pro-apoptotic activity in p53-Y220C mutant cancer cell lines, with minimal effects in wild-type or p53-null cells. p53 Activator 17 induces a mutant-to-wild-type conformational shift in cellular p53-Y220C, accompanied by transcriptional activation of canonical p53 target genes, including BBC3 (PUMA) and MDM2. p53 Activator 17 can be used for the study of hepatocellular carcinoma and breast cancer .
Cat. No.: HY-180618
p53 DUBTAC modulator-1 (Compound A1) is a p53 Y220C DUBTAC modulator (Kd = 12.09 µM). p53 DUBTAC modulator-1 effectively reactivates and deubiquitinates mutant p53 Y220C. p53 DUBTAC modulator-1 upregulates p53 Y220C protein levels. p53 DUBTAC modulator-1 induces Apoptosis, reduces Bcl-2, inhibits Wnt signaling. p53 DUBTAC modulator-1 has anti-cancer activity against liver cancer .
Cat. No.: HY-184518
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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.) .
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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
