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Cat. No.: 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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₅₀H₅₂ClN₉O₇S
분자량:958.52

보관:

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

Data Sheet (269 KB)

YT117R Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

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

분자량 958.52
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 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)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

견적 받기

Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

YT117R

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms