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Cat. No.: HY-146806

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YL93

YL93 is a dual inhibitors of MDM2/4 with K_i values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition.

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CAS No.: 2771313-42-7
Formule: C₃₇H₃₈Cl₂F₂N₄O₄
Masse moléculaire:711.62

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (277 KB)

YL93 Chemical Structure

CAS No.: 2771313-42-7

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Activité biologique
- Description
- Cellular Effect
- In Vitro
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	50.7 nM Compound: 31	Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human HCT-116 cells expressing wild type p53 and MDM2 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
HEK293	IC₅₀	6.25 μM Compound: 31	Cytotoxicity against HEK293 cells assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against HEK293 cells assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
HeLa	IC₅₀	7.37 μM Compound: 31	Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human HeLa cells harbouring unstable p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
MCF7	IC₅₀	0.52 μM Compound: 31	Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human MCF7 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
NCI-H460	IC₅₀	0.46 μM Compound: 31	Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human NCI-H460 cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
RKO	IC₅₀	0.2 μM Compound: 31	Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human RKO cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
SW480	IC₅₀	2.82 μM Compound: 31	Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human SW480 cells harbouring mutant p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]
U2OS	IC₅₀	0.37 μM Compound: 31	Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay Cytotoxicity against human U2OS cells expressing wild type p53 assessed as cell growth inhibition incubated for 4 days by CCK-8 assay	[PMID: 35420431]

In Vitro

YL93 shows anti-tumor activity and inhibits HCT-116 cell growth with an IC₅₀ value of 50.7 nM^[1].
YL93 (0.078-2.5 μM; 24 h) increases the protein level of p53, p21, MDM2^[1].
YL93 (0.02-2.5 μM; 24 h) arrests cell cycle at G1^[1].
YL93 (6.25-25 μM; 48 h) increases apoptotic RKO cells^[1].
YL93 (2.5 μM; 48 h) increases transcription of p53-targeted genes, MDM2, p21, and PUMA in MDM4-overexpressing cell lines H460, MCF-7, and U-2 OS^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HCT-116 cells
Concentration:

0.078125 μM, 0.15625 μM, 0.3125 μM, 0.625 μM, 1.25 μM, and 2.5 μM
Incubation Time:

24 hours
Result:

Significantly increased the protein level of p53, p21, MDM2.

Cell Cycle Analysis^[1]

Cell Line:

HCT-116 cells
Concentration:

0.02 μM, 0.1 μM, 0.5 μM, 2.5 μM
Incubation Time:

24 hours
Result:

Arrested cell cycle at G1 phase.

Chemical Information

CAS No. 2771313-42-7
Masse moléculaire 711.62
Formule C₃₇H₃₈Cl₂F₂N₄O₄
SMILES

FC(C(Cl)=CC=C1)=C1[C@@H]([C@@H](N[C@H]2CC(C)(C)C)C(NC3=CC=C(C=C3OC)C(O)=O)=O)[C@]2(C4=CC=C(Cl)C=C4F)CNCC5=CC=NC=C5
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang S, et al. Structure-Based Discovery of MDM2/4 Dual Inhibitors that Exert Antitumor Activities against MDM4-Overexpressing Cancer Cells. J Med Chem. 2022 Apr 28;65(8):6207-6230. [Content Brief]

Calculators

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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