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Art. -Nr.: HY-169148

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YT117R

YT117R is a PROTAC degrader targeting BRD4. YT117R binds stereoselectively and site-specifically to the cysteine residue C1113 of DCAF1 to form a covalent interaction. YT117R promotes BRD4 degradation via a DCAF1-dependent, proteasome- and cullin-RING E3 ligase-mediated process. YT117R exhibits stereoselective activity dependent on wild-type DCAF1, which is blocked by the DCAF1^C1113A mutation.
(Pink: BRD4 ligand (HY-78695); Blue: DCAF1 ligand (HY-158301); Black: linker (HY-42776)).

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Formel: C₅₀H₅₂ClN₉O₇S
Molecular Weight:958.52

Speicherung:

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

Data Sheet (269 KB)

YT117R Chemical Structure

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Verfügbarkeit

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

YT117R is a PROTAC degrader targeting BRD4. YT117R binds stereoselectively and site-specifically to the cysteine residue C1113 of DCAF1 to form a covalent interaction. YT117R promotes BRD4 degradation via a DCAF1-dependent, proteasome- and cullin-RING E3 ligase-mediated process. YT117R exhibits stereoselective activity dependent on wild-type DCAF1, which is blocked by the DCAF1^C1113A mutation^[1]. (Pink: BRD4 ligand (HY-78695); Blue: DCAF1 ligand (HY-158301); Black: linker (HY-42776)).

IC₅₀ & Target^[1]

BRD4

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In Vitro

YT117R stereoselectively engages C1113 of recombinant DCAF1, as shown by concentration-dependent blockade of MY-11B probe labeling in gel-ABPP assays^[1].
YT117R (0.05-1 μM; 12 h) induces concentration-dependent, stereoselective, and DCAF1_C1113-dependent degradation of BRD4 in DCAF1-WT-expressing HEK293T cells, with an activity dependent on the proteasome and cullin-RING E3 ligase pathway^[1].

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

Western Blot Analysis^[1]

Cell Line:

DCAF1-WT-expressing HEK293T cells
Concentration:

0.05 μM; 0.1 μM; 0.2 μM; 0.5 μM; 1 μM
Incubation Time:

12 h
Result:

Promoted concentration-dependent degradation of BRD4 in DCAF1-WT-expressing cells.
Induced submaximal degradation compared to positive control dBET6.
Showed stereoselective activity (not induced by YT117S).
Exhibited absent degradation in DCAF1-C1113A-expressing cells.
Had induced BRD4 degradation blocked by pre-treatment with MLN4924 and MG132.

Chemical Information

Molecular Weight 958.52
Formel C₅₀H₅₂ClN₉O₇S
SMILES

C=CC(N1C[C@@H]([C@@H]1C(NC2=CC=CC3=C2N=CC=C3)=O)C4=CC=C(C=C4)C(NCCOCCOCCOCCNC(C[C@@H]5N=C(C6=C(N7C(C)=NN=C57)SC(C)=C6C)C8=CC=C(C=C8)Cl)=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 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)
Handling Instructions (2659 KB)

Verweise

[1]. Tao Y, et al. Targeted Protein Degradation by Electrophilic PROTACs that Stereoselectively and Site-Specifically Engage DCAF1. Journal of the American Chemical Society. 2022 Oct 12;144(40):18688-18699. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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YT117R

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