2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain c-Myc
  4. PROTAC BET Degrader-14

PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma.
(Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-149452); Black: linker (HY-179587)).

For research use only. We do not sell to patients.

PROTAC BET Degrader-14

PROTAC BET Degrader-14 Chemical Structure

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PROTAC BET Degrader-14 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

PROTAC BET Degrader-14 is a highly efficient PROTAC targeting BET (bromodomain and extra-terminal domain). PROTAC BET Degrader-14 can degrade all BET (BRD2, BRD3, BRD4) family proteins. PROTAC BET Degrader-14 potently degrades BET proteins in U2OS osteosarcoma cell lines (BRD4 DC50 = 130 nM) and KYSE180 esophageal squamous cell carcinoma cell lines (DC50 = 40 nM). PROTAC BET Degrader-14’s dependence on the ubiquitin-proteasome system. PROTAC BET Degrader-14 decreases levels of BET-regulated gene products c-Myc, RUNX2, and KRT14. PROTAC BET Degrader-14 can be used for the study of osteosarcoma[1]. (Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-149452); Black: linker (HY-179587)).

IC50 & Target[1]

BRD4

130 nM (DC50)

BRD4

40 nM (DC50)

BRD2

 

BRD3

 

In Vitro

PROTAC BET Degrader-14 (Compound 105B) (0.01-10 μM, 24 h) dose-dependently degrades BRD4 in U2OS osteosarcoma cells[1].
PROTAC BET Degrader-14 (10 nM, 0-24 h) induces rapid degradation in U2OS osteosarcoma cells, although the effect may rebound due to BRD4 resynthesis[1].
PROTAC BET Degrader-14 (0.01 nM-1 μM, 24 h) reduces c-Myc and RUNX2 levels in U2OS osteosarcoma cells[1].
PROTAC BET Degrader-14 (0.51 nM-10) reduces KRT14 levels in KYSE180 esophageal squamous cell carcinoma cells but does not degrade BRDT[1].

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

PROTAC BET Degrader-14 Related Antibodies

Western Blot Analysis[1]

Cell Line: U2OS osteosarcoma cells
Concentration: 10 nM
Incubation Time: 0 h, 0.5 h, 1 h, 1.5 h, 2 h, 4 h, 6 h, 8 h, 24 h
Result: BRD4 degradation occurs within 4 hours and rebounds after 24 hours.
Molecular Weight

1161.80

Formula

C59H73ClN12O9S
SMILES

O=C(C[C@@H]1N=C(C2=CC=C(Cl)C=C2)C(C(C)=C(C)S3)=C3N4C1=NN=C4C)NCCOCCOCCOCCOCCOCCOCCOCCOCC5=CN(N=N5)C(C=C6)=CC7=C6C(NCCCNCC8=CC=C9C(C=CN9)=C8)=CC=N7
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PROTAC BET Degrader-14 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC BET Degrader-14PROTAC BET Degrader14PROTAC BET Degrader 14PROTACsEpigenetic Reader Domainc-MycMycPROTACUbiquitin-proteasome systemUPSRUNX2KRT14Inhibitorinhibitorinhibit

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