2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. PROTAC BET Degrader-16

PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia.
(Pink: BET Target protein ligand; Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W018678)).

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PROTAC BET Degrader-16

PROTAC BET Degrader-16 Chemical Structure

CAS No. : 2410947-65-6

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PROTAC BET Degrader-16 Related Antibodies

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Description

PROTAC BET Degrader-16 (Compound A10) is a BET PROTAC degrader with a DC50 of 0.31 nM against BRD4, and it preferentially targets BRD4 over other BET family members. PROTAC BET Degrader-16 degrades BRD2, BRD3 and BRD4 via the ubiquitin-proteasome system, a process that requires target binding and recruitment of the CRBN E3 ligase. PROTAC BET Degrader-16 induces cell cycle arrest and promotes apoptosis. PROTAC BET Degrader-16 exerts anti-tumor activity against acute myeloid leukemia[1]. (Pink: BET Target protein ligand; Blue: Cereblon ligand (HY-A0003); Black: linker (HY-W018678)).

IC50 & Target[1]

BRD4

0.31 nM (DC50)

BRD2

6.44 nM (DC50)

BRD3

7.93 nM (DC50)

Cereblon

 

In Vitro

PROTAC BET Degrader-16 binds directly to BRD4 (BD1) with an IC50 of 3.0 nM[1].
PROTAC BET Degrader-16 (72 h) potently inhibits the proliferation of MV4-11 leukemia cells with an IC50 value of 1.964 nM, while it exhibits low activity in RAMOS cells[1].
PROTAC BET Degrader-16 (0.1-300 nM; 1-24 h) efficiently and selectively degrades BRD2, BRD3 and BRD4 in a time- and concentration-dependent manner in MV4-11 cells, with a DC50 of 0.31 nM for BRD4. Its mechanism of action depends on BRD4 binding, CRBN recruitment, and the ubiquitin-proteasome system[1].
PROTAC BET Degrader-16 (1-100 nM) induces dose-dependent S-phase arrest in MV4-11 cells[1].
Treatment of MV4-11 cells with PROTAC BET Degrader-16 (0.3-100 nM; 48 h) for 48 h induces concentration-dependent apoptosis, and its activity is significantly higher than that of ABBV-075 (HY-100015)[1].

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

PROTAC BET Degrader-16 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.1-300 nM (concentration-dependent degradation); 100 nM (time-dependent degradation, complete degradation, mechanism studies)
Incubation Time: 24 h (concentration-dependent degradation, complete degradation, mechanism studies); 1, 2, 4, 8, 14, 24 h (time-dependent degradation)
Result: Induced nearly complete loss of BRD2, BRD3, and BRD4 protein at 100 nM for 24 h, with concurrent downregulation of c-Myc.
Exhibited a DC50 of 6.44 ± 0.18 nM for BRD2, 7.93 ± 0.73 nM for BRD3, and 0.31 ± 0.08 nM for BRD4.
Showed time-dependent degradation, with effects observed as early as 1 h post-treatment at 100 nM.
Abolished degradation completely when cells were pre-treated with ABBV-075, lenalidomide, MLN4924, MG132, or carfilzomib.
Parmacokinetics
Species Dose Route Cmax T1/2 MRT CL AUC0-∞
Mice[1] 1 mg/kg i.v. 888 ng/mL 0.143 h 0.104 h 195 mL/min/kg 94.8 ng·h/mL
Mice[1] 2 mg/kg i.p. 216 ng/mL 1.53 h 2.51 h / 481 ng·h/mL
In Vivo

PROTAC BET Degrader-16 (administered via i.p. injection once every 2 days for 21 days at doses of 2-6 mg/kg) exerts dose-dependent antitumor effects in the MV4-11 AML xenograft model[1].

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

Animal Model: Balb/c nude (4 to 5 weeks old; subcutaneous AML xenograft model)[1]
Dosage: 2 mg/kg; 6 mg/kg
Administration: i.p.; every other day; 21 days
Result: Achieved 48.8% tumor growth inhibition (TGI) and significantly downregulated BRD4 and c-Myc protein expression in tumor tissue compared to vehicle control at 2 mg/kg.
Achieved 76.2% TGI, with a more pronounced reduction in c-Myc protein expression than the 2 mg/kg dose at 6 mg/kg.
Caused no significant body weight loss in treated mice.
Resulted in no significant changes in hepatic (ALT, AST), renal, or cardiac (CK-MB, LDH) toxicity biomarkers compared to vehicle control at both doses.
Molecular Weight

885.93

Formula

C44H45F2N7O9S
CAS No.
SMILES

O=C(C(N1)=CC(C(C2=CC(NS(=O)(CC)=O)=CC=C2OC3=CC=C(F)C=C3F)=CN4C)=C1C4=O)NCCCCCCCC(NC5=CC=CC6=C5CN(C(CC7)C(NC7=O)=O)C6=O)=O
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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-16 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-162410947-65-6PROTAC BET Degrader16PROTAC BET Degrader 16PROTACsEpigenetic Reader DomainApoptosisBRD3BRD4BRD2MV4-11 cellsJurkat leukemia cellsCRBN E3 ligaseubiquitin-proteasome systemacute myeloid leukemiaxenograft mouse modelsBET familyInhibitorinhibitorinhibit

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