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Cat. No.: HY-181869

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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.

CAS No.: 2409674-38-8
Formula: C₅₂H₅₇F₂N₁₁O₁₀S₂
Molecular Weight:1098.20

Storage:

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

PROTAC BET Degrader-17 Chemical Structure

CAS No.: 2409674-38-8

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Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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

All PROTACs Isoforms :

All Epigenetic Reader Domain Isoforms :

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.

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	AUC_0-∞	C_max	T_1/2	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.

Chemical Information

CAS No. 2409674-38-8
Molecular Weight 1098.20
Formula C₅₂H₅₇F₂N₁₁O₁₀S₂
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

Handling Instructions (2659 KB)

References

[1]. Wei Q, et al. Design and evaluation of selective BET PROTACs with potent antitumor efficacy and safety against acute myeloid leukemia. Eur J Med Chem. 2026;308:118667. [Content Brief]

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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.

MOQ

Minimum order quantity

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PROTAC BET Degrader-17

All PROTACs Isoforms

All Epigenetic Reader Domain Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

PROTAC BET Degrader-17 Related Classifications

HY-181869 Related Classifications