PROTAC BRD4 Degrader-39
PROTAC BRD4 Degrader-39 is a selective targeting Bromodomain protein 4 (BRD4) degrader with an DC50 value of 24.66 nM. PROTAC BRD4 Degrader-39 conjugates BRD PROTAC (ARV-771) (HY-100972) with carbohydrate. PROTAC BRD4 Degrader-39 selectively delivers to tumor cells with high GLUT1 expression, followed by GSH-triggered release of ARV-771 and degrades BRD4. PROTAC BRD4 Degrader-39 can inhibit tumor growth and show no significant toxicity. PROTAC BRD4 Degrader-39 can be used for the research of cancer, such as breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: linker (HY-42427)).
For research use only. We do not sell to patients.
- Formula: C63H81ClN12O15S4
- Molecular Weight:1410.10
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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BRD4 24.66 nM (DC50) |
VHL |
PROTAC BRD4 Degrader-39 (Compound NG-2) (0.01-10 μM, 3-48 h) degrades BRD4 in a concentration- and time-dependent manner in MDA-MB-231 cells[1].
PROTAC BRD4 Degrader-39 degrades BRD4 depending on GLUTs and proteasome in MDA-MB-231 cells[1].
PROTAC BRD4 Degrader-39 (5-5000 nM, 3 h) degrades BRD4 in MDA-MB-157, MCF-7, T-47D and BEAS-2B cells[1].
PROTAC BRD4 Degrader-39 is difficult to be recognized by P-gp, thereby effectively evading the efflux effect in Caco-2 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.01, 0.1, 1 and 10 μM
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Incubation Time:3, 6, 12, 24 and 48 h
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Result:Degraded BRD4 in a concentration- and time-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 tumor mice models[1]
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Dosage:2.5 mg/kg
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Administration:Intraperitoneally injection, every other day for 14 times
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Result:Reduced tumor volume and weight.
Reduced BRD4 levles and Ki67-positive cells.
Had no changes of body weight, AST/ALT and BUN/Scr.
Chemical Information
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Molecular Weight 1410.10
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Formula C63H81ClN12O15S4
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SMILES
CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@H](C4=NN=C(N42)C)CC(NCCOCCCOCC(N[C@H](C(N5C[C@@H](C[C@H]5C(N[C@@H](C)C6=CC=C(C=C6)C7=C(C)N=CS7)=O)OC(OCCSSCCN8C=C(N=N8)CO[C@@H]([C@@H]9O)O[C@H](CO)[C@H](O)C9O)=O)=O)C(C)(C)C)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PROTAC BRD4 Degrader-39 Related Classifications
HY-175767 Related Classifications
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