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Art. -Nr.: HY-172562

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BTR2004

Name: BTR2004
Brand: MedChemExpress
SKU: HY-172562
Price: 1000.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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BTR2004 is a potent and selective BET family (BRD2/3/4) PROTAC degrader, with EC₅₀ values of 46, 87, and 777 nM, respectively. By bridging BET family proteins and the CUL3-KLHL20 E3 ubiquitin ligase, BTR2004 forms a ternary complex in the nucleus, thereby mediating the degradation of target proteins via the ubiquitin-proteasome system. BTR2004 can be used in research related to prostate cancer, breast cancer, colorectal cancer, osteosarcoma, and hepatocellular carcinoma.
(Pink: BET ligand (HY-161125); Blue: KLHL20 ligand (HY-172563); Black: linker (HY-W015236)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit : 99.86%
CAS. Nr.: 3093583-69-5
Formel: C₅₄H₆₆ClN₁₃O₁₁S₃
Molecular Weight:1204.83

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BTR2004 Chemical Structure

CAS. Nr.: 3093583-69-5

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BTR2004 is a potent and selective BET family (BRD2/3/4) PROTAC degrader, with EC₅₀ values of 46, 87, and 777 nM, respectively. By bridging BET family proteins and the CUL3-KLHL20 E3 ubiquitin ligase, BTR2004 forms a ternary complex in the nucleus, thereby mediating the degradation of target proteins via the ubiquitin-proteasome system. BTR2004 can be used in research related to prostate cancer, breast cancer, colorectal cancer, osteosarcoma, and hepatocellular carcinoma^[1]^[2]. (Pink: BET ligand (HY-161125); Blue: KLHL20 ligand (HY-172563); Black: linker (HY-W015236)).

IC₅₀ & Target

^[1]

BRD2

46 nM (EC₅₀)

BRD3

87 nM (EC₅₀)

BRD4

777 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
PC-3	EC50	46 nM	Degradation of BRD2 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model. Degradation of BRD2 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.	36328355
PC-3	EC50	87 nM	Degradation of BRD3 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model. Degradation of BRD3 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.	36328355
PC-3	EC50	777 nM	Degradation of BRD4 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model. Degradation of BRD4 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.	36328355

In Vitro

Anti-cancerOthers

Anti-cancer

BTR2004 (62.5 nM-10 μM; 4 h) dose-dependently degrades BRD2, BRD3, and BRD4 proteins in PC3 cells, with EC₅₀ values of 46, 87, and 777 nM, respectively; it degrades nuclear BRD3 protein in the nuclear fraction of PC3 cells; and it degrades BRD3 protein in MDA-MB-231, HCT116, CAPAN-2, HepG2, and U2OS cells^[1].
BTR2004 (1.25-10 μM; 24-96 h) inhibits cell proliferation in PC3, MDA-MB-231 and HepG2 cells, and exhibits low cytotoxicity in the normal human cell line hTERT-BJ1^[1].
BTR2004 (2-8 μM; 45 min-3 h) induces time-dependent degradation of BRD2 and BRD4 via the ubiquitin-proteasome pathway in U2OS T-REx cells^[2].

Others

BTR2004 (12 μM; 3 h) acts to form a KLHL20-BTR2004-BRD4 ternary complex in the nucleus of U2OS T-REx cells expressing HA-KLHL20^[2].
BTR2004 retains the ability to degrade BRD2 in U2OS T-REx cells even in the presence of the nuclear export inhibitor KPT276 (HY-17539)^[2].

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

Western Blot Analysis^[1]

Cell Line:

PC3 cells
Concentration:

62.5 nM, 125 nM, 250 nM, 500 nM, 1 μM, 2 μM, 10 μM
Incubation Time:

4 h
Result:

Degraded BRD2, BRD3, and BRD4 proteins, as well as BRD3 protein in the nuclear fraction.
Degraded BRD2, BRD3, and BRD4 proteins in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231, HCT116, U2OS, CAPAN-2, HepG2 cells
Concentration:

10 μM (MDA-MB-231, HCT116, U2OS); 5 μM (CAPAN-2, HepG2)
Incubation Time:

4 h
Result:

Degraded BRD3 protein.

Cell Viability Assay^[1]

Cell Line:

PC3, MDA-MB-231, HepG2, hTERT-BJ1 cells
Concentration:

1.25 μM, 2.5 μM, 5 μM, 10 μM
Incubation Time:

24, 72, 96 h
Result:

Significantly inhibited the growth and proliferation of cancer cells.
Exhibited low cytotoxicity to hTERT-BJ1 normal human cell line.

Related Protocols :

Chemical Information

CAS. Nr. 3093583-69-5
Appearance Solid
Molecular Weight 1204.83
Formel C₅₄H₆₆ClN₁₃O₁₁S₃
Color White to off-white
SMILES

CC1=NN=C2N1C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NCC(NCC(NCC(N[C@H](C(N5[C@H](C(N[C@@H](CC(O)=O)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)CSC6)=O)=O)=O)CCC5)=O)CSCC7=CC=CC6=C7)=O)=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (83.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8300 mL

4.1500 mL

8.2999 mL

5 mM

0.1660 mL

0.8300 mL

1.6600 mL

10 mM

0.0830 mL

0.4150 mL

0.8300 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (294 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Farrell BM, et al. A synthetic KLHL20 ligand to validate CUL3 as a potent E3 ligase for targeted protein degradation. Genes & development. 2022 Sep 01;36(17-18):1031-1042. [Content Brief]

[2]. Fechtmeyer PH, et al. Temporal and Spatial Characterization of CUL3-Driven Targeted Degradation of BET Family BRD Proteins by the Macrocycle-Based Degrader BTR2004. ACS chemical biology. 2025 Sep 19;20(9):2056-2062.

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.8300 mL	4.1500 mL	8.2999 mL	20.7498 mL
	5 mM	0.1660 mL	0.8300 mL	1.6600 mL	4.1500 mL
	10 mM	0.0830 mL	0.4150 mL	0.8300 mL	2.0750 mL
	15 mM	0.0553 mL	0.2767 mL	0.5533 mL	1.3833 mL
	20 mM	0.0415 mL	0.2075 mL	0.4150 mL	1.0375 mL
	25 mM	0.0332 mL	0.1660 mL	0.3320 mL	0.8300 mL
	30 mM	0.0277 mL	0.1383 mL	0.2767 mL	0.6917 mL
	40 mM	0.0207 mL	0.1037 mL	0.2075 mL	0.5187 mL
	50 mM	0.0166 mL	0.0830 mL	0.1660 mL	0.4150 mL
	60 mM	0.0138 mL	0.0692 mL	0.1383 mL	0.3458 mL
	80 mM	0.0104 mL	0.0519 mL	0.1037 mL	0.2594 mL

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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BTR2004

Biologische Aktivität

Beschreibung

IC50 & Target

Cellular Effect

In Vitro

Chemical Information

Lösungsmittel & Löslichkeit

In Vitro:

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BTR2004 Related Classifications

HY-172562 Related Classifications

Bioz

Keywords

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