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Cat. No.: HY-176035

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MS479

MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: K_d = 200 nM; GLP: K_d = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells.
(Pink: BRD4 ligand (HY-78695); Blue: SPOP ligand (HY-176036); Black: linker (HY-176037)).

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화학식: C₅₉H₈₂ClN₁₁O₅S
분자량:1092.87

보관:

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

Data Sheet (270 KB)

MS479 Chemical Structure

사이즈

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

제품 설명

MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: K_d = 200 nM; GLP: K_d = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells^[1]. (Pink: BRD4 ligand (HY-78695); Blue: SPOP ligand (HY-176036); Black: linker (HY-176037)).

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

In Vitro

MS479 (Compound 9) (0.5-5 μM, 24 h) shows the best degradation of BRD4 (S) (>50% degradation at 5 μM) in HT29 cell line^[1].
MS479 (0.156-10 μM, 24 h) shows relatively weak effect on the BRD4 (L) protein level (DC₅₀ = 13.2 μM), with approximately 50% degradation at 10 μM in HT29 cell line^[1].
MS479 (1-10 μM, 24 h) regulates the BRD4 protein level through a post-translational mechanism in HT29 cell line^[1].
MS479 (5 μM, 24 h) suggests the degradation of BRD4 (S) is dependent on BRD4, GLP, SPOP, and UPS engagement in HT29 cell line^[1].
MS479 (0.021-10 μM, 72 h) displays a significant antiproliferative effect (GI₅₀ = 4.5 μM) in a concentration-dependent manner in HT29 cells but not cytotoxic to normal cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

HT29
Concentration:

1-10 μM
Incubation Time:

2-72 h
Result:

Observed degradation of BRD4 (S) at 16 h and persisted up to 72 h.
Required longer time (48 h or longer) to degrade BRD4 (L), BRD3, and BRD2 effectively.
Reduced c-Myc protein level sharply after 2 h and completely abolished at 16 h.

Western Blot Analysis^[1]

Cell Line:

Biotin-MS479 (20 or 100 μM), parent BRD4 ligand (JQ1 (HY-13030), 1 μM), parent GLP ligand (MS1262, 1 μM) or a neddylation inhibitor (MLN4924 (HY-70062), 1 μM) pre-treated HT29 cell lines
Concentration:

5 μM
Incubation Time:

24 h
Result:

Rescued BRD4 (S) degradation by pretreatment of HT29 cells.
Induced BRD4 degradation in HT29 cells, but the negative controls (MS479N1 and MS479N2) did not.
Showed BRD4 (S), BRD4 (L), and GLP all coeluted with SPOP in the presence of Biotin MS479, suggesting MS479 indeed induces the interaction between BRD4 and the GLP-SPOP complex.

Chemical Information

분자량 1092.87
화학식 C₅₉H₈₂ClN₁₁O₅S
SMILES

CC1=NN=C2[C@@H](N=C(C3=C(N21)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCCCCCCCCCNC(CCCN5CCC(NC6=C7C=C(OC)C(OCCCN8CCCC8)=CC7=NC(N9CCOCC9)=C6)CC5)=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 (270 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]. Deng Z, et al., Harnessing the SPOP E3 Ubiquitin Ligase via a Bridged Proteolysis Targeting Chimera (PROTAC) Strategy for Targeted Protein Degradation. J Med Chem. 2025 Apr 24;68(8):8634-8647. [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.

Keywords

MOQ

Minimum order quantity

100 mg

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

상품명:
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MS479

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

MS479 Related Classifications

HY-176035 Related Classifications