Art. -Nr.: HY-103633

PROTAC BET Degrader-1

Name: PROTAC BET Degrader-1
Brand: MedChemExpress
SKU: HY-103633
Price: 550.00 USD
Availability: InStock
Rating: 5 (2 reviews)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

PROTAC BET Degrader-1 is a BRD2/BRD3/BRD4 PROTAC degrader. PROTAC BET Degrader-1 inhibits the growth of acute leukemia cells. PROTAC BET Degrader-1 is applicable to the research of acute leukemia.
(Pink: BRD2 and BRD3 and BRD4 ligand (HY-112429); Blue: Cereblon ligand (HY-42771); Black: linker).

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Reinheit : 99.41%
CAS. Nr.: 2093386-22-0
Formel: C₄₄H₄₅N₁₁O₉
Molecular Weight:871.90

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PROTAC BET Degrader-1 Chemical Structure

CAS. Nr.: 2093386-22-0

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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
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PROTAC BET Degrader-1 is a BRD2/BRD3/BRD4 PROTAC degrader. PROTAC BET Degrader-1 inhibits the growth of acute leukemia cells. PROTAC BET Degrader-1 is applicable to the research of acute leukemia^[1]. (Pink: BRD2 and BRD3 and BRD4 ligand (HY-112429); Blue: Cereblon ligand (HY-42771); Black: linker).

IC₅₀ & Target

^[1]

BRD2

BRD3

BRD4

Cereblon

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Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	45.5 nM Compound: 9	Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]
RS4-11	IC₅₀	4.3 nM Compound: 9	Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]

In Vitro

Anti-cancer

PROTAC BET Degrader-1 (Compound 9) (4 days) potently inhibits the proliferation of RS4;11 and MOLM-13 acute leukemia cells, with IC₅₀ values of 4.3 and 45.5 nM^[1].
PROTAC BET Degrader-1 (3-30 nM; 3 hours) effectively degrades BRD2, BRD3 and BRD4 proteins in RS4;11 acute leukemia cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

human acute leukemia RS4;11 cells
Concentration:

3 nM, 10 nM, 30 nM
Incubation Time:

3 hours
Result:

Effectively decreased the levels of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at concentrations as low as 3-10 nM, whereas the BET inhibitor 8 showed no degradation effect at 100 nM and 300 nM.

Chemical Information

CAS. Nr. 2093386-22-0
Appearance Solid
Molecular Weight 871.90
Formel C₄₄H₄₅N₁₁O₉
Color Light yellow to yellow
SMILES

CCN1C(NC2=C3C4=CC(OC)=C(C(C(C)=NO5)=C5C)C=C4NC3=NC(C(NCCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)=O)=N2)=CC(C9CC9)=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

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Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
ACS Pharmacol Transl Sci

General Stepwise Approach to Optimize a TR-FRET Assay for Characterizing the BRD/PROTAC/CRBN Ternary Complex. [Abstract]

2021 Feb 26;4(2):941-952. PMID: 33860212

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 50 mg/mL (57.35 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

1.1469 mL

5.7346 mL

11.4692 mL

5 mM

0.2294 mL

1.1469 mL

2.2938 mL

10 mM

0.1147 mL

0.5735 mL

1.1469 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.67 mg/mL (1.92 mM); Clear solution

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.67 mg/mL (1.92 mM); Suspended solution

This protocol yields a suspended solution of ≥ 1.67 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. Journal of medicinal chemistry. 2018 Jan 25;61(2):462-481. [Content Brief]

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.1469 mL	5.7346 mL	11.4692 mL	28.6730 mL
	5 mM	0.2294 mL	1.1469 mL	2.2938 mL	5.7346 mL
	10 mM	0.1147 mL	0.5735 mL	1.1469 mL	2.8673 mL
	15 mM	0.0765 mL	0.3823 mL	0.7646 mL	1.9115 mL
	20 mM	0.0573 mL	0.2867 mL	0.5735 mL	1.4337 mL
	25 mM	0.0459 mL	0.2294 mL	0.4588 mL	1.1469 mL
	30 mM	0.0382 mL	0.1912 mL	0.3823 mL	0.9558 mL
	40 mM	0.0287 mL	0.1434 mL	0.2867 mL	0.7168 mL
	50 mM	0.0229 mL	0.1147 mL	0.2294 mL	0.5735 mL

Bioz

Keywords

PROTAC BET Degrader-1

2 Cited Publications

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PROTAC BET Degrader-1

Publications Citing Use of MedChemExpress (MCE) PROTAC BET Degrader-1

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