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Cat. No.: HY-176035

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MS479

MS479 is a PROTAC degrader targeting BRD4, BRD3 and BRD2. MS479 recruits the E3 ligase SPOP by bridging the protein GLP, thereby promoting polyubiquitination modification and subsequent 26S proteasomal degradation. MS479 inhibits the proliferation of colorectal cancer cells and can be used for research on colorectal cancer and triple-negative breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: SPOP ligand (HY-176036); Black: linker (HY-176037)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₅₉H₈₂ClN₁₁O₅S
분자량:1092.87

보관:

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

Data Sheet (277 KB)

MS479 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

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

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

Biological Activity

제품 설명

MS479 is a PROTAC degrader targeting BRD4, BRD3 and BRD2. MS479 recruits the E3 ligase SPOP by bridging the protein GLP, thereby promoting polyubiquitination modification and subsequent 26S proteasomal degradation. MS479 inhibits the proliferation of colorectal cancer cells and can be used for research on colorectal cancer and triple-negative breast cancer^[1]. (Pink: BRD4 ligand (HY-78695); Blue: SPOP ligand (HY-176036); Black: linker (HY-176037)).

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	DC₅₀	6.2 μM	Degradation of BRD4 short isoform (BRD4 (S)) in human HT29 colorectal cancer cells assessed via Western blot-based protein degradation assay incubated for 24 hrs. Degradation of BRD4 short isoform (BRD4 (S)) in human HT29 colorectal cancer cells assessed via Western blot-based protein degradation assay incubated for 24 hrs.	40202531
HT-29	GI50	4.5 μM	Antiproliferative activity against human HT29 colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay. Antiproliferative activity against human HT29 colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by WST-8 assay.	40202531

In Vitro

MS479 binds with high affinity to purified recombinant BRD4-BD2 (K_D=200 nM) and GLP-SET domain (K_D=306 nM)^[1].
MS479 (0.156-10 μM; 2-72 h) induces concentration- and time-dependent degradation of BRD4 (S), weak degradation of BRD4 (L), BRD3, and BRD2, and potent suppression of c-MYC in HT29 cells, with BRD4 (S) degradation dependent on BRD4, GLP, and the ubiquitin-proteasome system^[1].
MS479 (1-10 μM; 24 h) regulates BRD4, BRD3, and BRD2 protein levels via a post-translational mechanism and downregulates c-MYC transcription in HT29 cells^[1].
MS479 (0.1-5 μM; 24 h) degrades BRD4 (S), BRD3, BRD2, and BRD4 (L) in MDA-MB-231 cells, with greater activity against BRD4 (L) than in HT29 cells^[1].
MS479 (0.021-10 μM; 72 h) potently inhibits proliferation of HT29 colorectal cancer cells (GI₅₀=4.5 μM) without affecting viability of normal PNT2 prostatic epithelial 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 colorectal cancer cells
Concentration:

0.156-10 μM (24 h); 5 μM (2 h, 4 h, 8 h, 16 h, 48 h, 72 h); 1 μM (pretreatment with MS1262, JQ1, MLN4924)
Incubation Time:

2 h (pretreatment); 2 h, 4 h, 8 h, 16 h, 24 h, 48 h, 72 h (MS479 treatment)
Result:

Induced >50% degradation of BRD4 short isoform (BRD4 (S)) at 5 μM for 24 h.
Induced degradation of BRD4 (S) with a DC₅₀ of 6.2 μM and maximum degradation (D_max) of 63% in concentration-dependent testing.
Induced ~50% degradation of BRD4 long isoform (BRD4 (L)), weak degradation of BRD3 and BRD2, and complete suppression of c-MYC at 10 μM for 24 h.
Induced BRD4 (S) degradation detectable at 16 h and persisting to 72 h in time-dependent testing.
Required 48 h or longer for effective degradation of BRD4 (L), BRD3, and BRD2 in time-dependent testing.
Caused c-MYC levels to drop sharply starting at 2 h in time-dependent testing.
Degradation of BRD4 (S) was rescued by pretreatment with MS1262, JQ1, or MLN4924.

Real Time qPCR^[1]

Cell Line:

HT29 colorectal cancer cells
Concentration:

1-10 μM
Incubation Time:

24 h
Result:

Did not alter mRNA levels of BRD4 (S), BRD4 (L), BRD3, or BRD2.
Significantly downregulated c-MYC mRNA at 5 μM and 10 μM.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 triple-negative breast cancer cells
Concentration:

0.1-5 μM
Incubation Time:

24 h
Result:

Induced degradation of BRD4 (S), BRD3, and BRD2.
Showed enhanced activity against BRD4 (L) compared to HT29 cells.

Cell Viability Assay^[1]

Cell Line:

HT29 colorectal cancer cells, PNT2 normal prostatic epithelial cells
Concentration:

0.021-10 μM
Incubation Time:

72 h
Result:

Inhibited HT29 cell proliferation with a GI₅₀ of 4.5 μM.
Did not suppress proliferation of PNT2 cells at any tested concentration.

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 (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)
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. Journal of medicinal chemistry. 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

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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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Amount: USD 0.00

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

상품명:
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수량:
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상품명:
CAS No.:
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수량:

MS479

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms