2. PROTAC Epigenetics Apoptosis
  3. PROTACs Epigenetic Reader Domain Apoptosis
  4. PROTAC BET Degrader-17

PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia.

(Pink: BET ligand (HY-169980); Blue: VHL ligand (HY-125845); Black: linker (HY-108369)).

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

PROTAC BET Degrader-17

PROTAC BET Degrader-17 Chemical Structure

CAS No. : 2409674-38-8

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PROTAC BET Degrader-17 Related Antibodies

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Description

PROTAC BET Degrader-17 is a potent BET protein PROTAC degrader. By recruiting the VHL E3 ligase, PROTAC BET Degrader-17 specifically degrades BRD2, BRD3 (DC50=0.09 nM) and BRD4 (IC50=4.3 nM). PROTAC BET Degrader-17 exhibits strong anti-tumor activity in acute myeloid leukemia (AML) studies; it not only inhibits cancer cell proliferation, induces cell cycle arrest and apoptosis, but also effectively suppresses tumor growth in xenograft mouse models. PROTAC BET Degrader-17 can be used to explore targeted therapies for acute myeloid leukemia[1].
(Pink: BET ligand (HY-169980); Blue: VHL ligand (HY-125845); Black: linker (HY-108369)).

IC50 & Target

VHL

 

BRD4

4.3 nM (IC50)

BRD3

0.09 nM (DC50)

BRD2

 

In Vitro

PROTAC BET Degrader-17 (Compound A12) inhibits the proliferation of MV4-11, RAMOS, K562 and Jurkat cells, with IC50 (72 h) values of 0.570 nM, 15.78 nM, 57.23 nM and 0.621 nM, respectively[1].
PROTAC BET Degrader-17 (0.1-300 nM; 15 min-24 h) induces the degradation of BRD2, BRD3 and BRD4 in a time- and dose-dependent manner, and downregulates c-Myc in MV4-11 cells[1].
PROTAC BET Degrader-17 (0.3-30 nM; 48 h) induces dose-dependent G1 cell cycle arrest in MV4-11 cells[1].
PROTAC BET Degrader-17 (0.3-100 nM; 48 h) induces dose-dependent apoptosis in MV4-11 cells, and exhibits superior potency over ABBV-075 (HY-100015) at concentrations below 10 nM[1].
PROTAC BET Degrader-17 exhibits excellent metabolic stability in mouse liver microsomes, with a half-life of 43.88 min and an intrinsic clearance rate of 31.59 mL/min/kg[1].

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

PROTAC BET Degrader-17 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.3-30 nM
Incubation Time: 48 h
Result: Induced dose-dependent G1 phase cell cycle arrest; as the concentration of PROTAC BET Degrader-17 increased, the percentage of cells in G1 phase increased.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0.3-100 nM
Incubation Time: 48 h
Result: Induced dose-dependent apoptosis; at lower concentrations (<10 nM), PROTAC BET Degrader-17 was more potent at inducing apoptosis than ABBV-075, though it did not achieve the maximal apoptotic induction level of A10.
Parmacokinetics
Species Dose Route AUC0-∞ Cmax T1/2 CL MRT
Mice[1] 1 mg/kg i.v. 1016 ng·h/mL 12403 ng/mL 0.317 h 17.0 mL/min/kg 0.0947 h
Mice[1] 2 mg/kg i.p. 1054 ng·h/mL 581 ng/mL 2.04 h / 2.50 h
In Vivo

PROTAC BET Degrader-17 (Compound A12) (2 mg/kg; i.p.; every other day; 21 days) achieves 60.5% tumor growth inhibition in MV4-11 AML xenografts with no significant body weight loss[1].

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

Animal Model: Balb/c nude mice (4 to 5 weeks old)[1]
Dosage: 2 mg/kg
Administration: i.p.; every other day; 21 days
Result: Achieved 60.5% tumor growth inhibition (TGI) relative to vehicle control.
Downregulated BRD4 and c-Myc protein expression in tumor tissue compared to vehicle control.
Caused no significant body weight loss during the study.
Molecular Weight

1098.20

Formula

C52H57F2N11O10S2
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)NCC5=CN(CCOCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)N=N5
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-17 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-172409674-38-8PROTAC BET Degrader17PROTAC BET Degrader 17PROTACsEpigenetic Reader DomainApoptosisubiquitin-proteasome systemBRD2acute myeloid leukemia cellsBRD3MV4-11 cellsVHL E3 ligaseBRD4acute myeloid leukemia xenograft mouse modelsJurkat cellsRAMOS cellsInhibitorinhibitorinhibit

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