dBET1

Name: dBET1
Brand: MedChemExpress
SKU: HY-101838
Rating: 5.0 (20 reviews)

Cat. No.: HY-101838 Purity: 98.96%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker).

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

CAS No. : 1799711-21-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of dBET1:

dBET1 (Standard) Get quote

20 Publications Citing Use of MCE dBET1

Flow Cytometry

: dBET1 purchased from MedChemExpress. Usage Cited in: Nature. 2024 Nov;635(8038):434-443. [Abstract]; Western blot analysis of liver tissue showed the expression of endogenous long and short BRD4 subtypes after treatment with a carrier or the small molecule BET protein degrader dBET1 (50 mg/kg).

: dBET1 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2024 Apr 4;84(7):1304-1320.e16. [Abstract]; Representative Western blots show the protein levels shown in the model breast cancer cell line MDA-MB-468, which was treated with the PROTACs (dBET1: 500 nM; 2 h) or DMSO shown, and after ectopic expression of UBE2R1 or UBE2R2.

: dBET1 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jun 1;80(11):2380-2393. [Abstract]; The cell lines shown were treated with DMSO, 100 nmol/L ZBC260, 500 nmol/L dBET1, or 1000 nmol/L JQ-1 for 24 or 48 hours, respectively. Annexin V/flow cytometry was used to detect the lysis of PARP and caspase in cell samples exposed to the drugs for 24 hours to assess apoptosis.

: dBET1 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jun 1;80(11):2380-2393. [Abstract]; The cell lines shown were treated with DMSO, 100 nmol/L ZBC260, 500 nmol/L dBET1, or 1000 nmol/L JQ-1 for 24 or 48 hours, respectively. Western blotting was used to assess the lysis of PARP and caspase in cell samples exposed to the drugs for 24 hours to evaluate apoptosis.

: dBET1 purchased from MedChemExpress. Usage Cited in: Cancer Res. 2020 Jun 1;80(11):2380-2393. [Abstract]; Before adding 100 nmol/L ZBC260 or 500 nmol/L dBET1, H157 cells were pretreated with 5 μmol/L MG132 for 30 minutes. Four hours later, the cells were collected for the preparation of whole-cell protein lysis buffer.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

dBET1 is a PROTAC connected by ligands for Cereblon and BRD4 with an EC₅₀ of 430 nM. dBET1 is a PROTAC that composes of (+)-JQ1 (HY-13030) linked to NSC 527179 (HY-14658) with a linker^[1]. (Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-103597); Black: linker).

IC₅₀ & Target

BRD4

430 nM (EC₅₀)

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	12.3 μM Compound: 1; dBET1	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
HEK293	IC₅₀	0.056 μM Compound: dBET1; D2B sythesis	Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay	[PMID: 35859867]
HEK293	IC₅₀	0.09 μM Compound: 1; dBET1	Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay Cytotoxicity against permeabilized HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay	[PMID: 35859867]
HEK293	IC₅₀	0.93 μM Compound: dBET1; D2B sythesis	Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay	[PMID: 35859867]
HEK293	IC₅₀	2.2 μM Compound: 1; dBET1	Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability incubated for 30 mins in presence of CRBN-tracer by nanoBRET assay	[PMID: 35859867]
HGC-27	IC₅₀	0.88 μM Compound: 1; dBET1	Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human HGC-27 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
HN-6	IC₅₀	7.07 μM Compound: dBET1	Antiproliferative activity against human HN-6 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay Antiproliferative activity against human HN-6 cells assessed as reduction in cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 34119833]
HeLa	IC₅₀	16.06 μM Compound: 1; dBET1	Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
HepG2	IC₅₀	19.8 μM Compound: 1; dBET1	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
MCF7	IC₅₀	5.3 μM Compound: 1; dBET1	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 4 days by CCK-8 assay	[PMID: 37084596]
MM1.S	IC₅₀	0.141 μM Compound: dBET1	Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MM1.S	IC₅₀	2469 nM Compound: 1; dBET1	Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay Antiproliferative activity against human MM1.S cells assessed as cell growth inhibition measured after 4 days by CellTitre-Glo assay	[PMID: 37084596]
MOLM-13	IC₅₀	140 nM Compound: d-BET1	Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
MOLM-13	IC₅₀	657 nM Compound: 4; dBET1	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]
MV4-11	IC₅₀	0.013 μM Compound: dBET1	Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay	[PMID: 36563515]
MV4-11	IC₅₀	11.8 nM Compound: 1; dBET1	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 3 days by CellTitre-Glo assay	[PMID: 37084596]
MV4-11	IC₅₀	42 nM Compound: d-BET1	Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
MV4-11	IC₅₀	6.1 nM Compound: dBET1	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo assay	[PMID: 37178483]
PC-3	EC₅₀	50 nM Compound: dBET-1	Cytotoxicity against human PC-3 cells assessed as reduction in cell viability measured after 5 days by Cell-Titer glo assay Cytotoxicity against human PC-3 cells assessed as reduction in cell viability measured after 5 days by Cell-Titer glo assay	[PMID: 36577036]
RS4-11	IC₅₀	78.8 nM Compound: 4; dBET1	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]
RS4-11	IC₅₀	79 nM Compound: d-BET1	Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]

In Vitro

Treatment with dBET1 down regulates MYC and PIM1 transcription. Degradation of BRD4 by dBET1 is associated with a more potent apoptotic consequence in MV4;11 cell line. Significantly increased apoptosis after only 4 h of dBET1 treatment is enhanced at 8 h. dBET1 also induces a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC₅₀= 0.14 μM, compare to IC₅₀= 1.1 μM with JQ1)^[1].

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

In Vivo

Administration of dBET1 attenuates tumor progression as determined by serial volumetric measurement, and decreases tumor weight assessed post-mortem. Acute pharmacodynamic degradation of BRD4 is observed four hours after a first or second daily treatment with dBET1 (50 mg/kg IP). A statistically significant destabilization of BRD4, down regulation of MYC and inhibition of proliferation is observed with dBET1 compare to vehicle control in excised tumors. Two weeks of dBET1 is well tolerated by mice without a meaningful effect on weight, white blood count, hematocrit or platelet count^[1].

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

Molecular Weight

785.27

Formula

C₃₈H₃₇ClN₈O₇S

CAS No.

1799711-21-9

Appearance

Solid

Color

White to light yellow

SMILES

O=C(NCCCCNC(COC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)=O)C[C@H]4C5=NN=C(C)N5C6=C(C(C)=C(C)S6)C(C7=CC=C(Cl)C=C7)=N4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 43.33 mg/mL (55.18 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.2734 mL	6.3672 mL	12.7345 mL
5 mM	0.2547 mL	1.2734 mL	2.5469 mL
10 mM	0.1273 mL	0.6367 mL	1.2734 mL

View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 90% Corn Oil
Solubility: ≥ 3 mg/mL (3.82 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.24%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (253 KB) HNMR (214 KB) LCMS (477 KB)

Handling Instructions (2659 KB)

References

[1]. Winter GE, et al. DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation. Science. 2015 Jun 19;348(6241):1376-81. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.2734 mL	6.3672 mL	12.7345 mL	31.8362 mL
	5 mM	0.2547 mL	1.2734 mL	2.5469 mL	6.3672 mL
	10 mM	0.1273 mL	0.6367 mL	1.2734 mL	3.1836 mL
	15 mM	0.0849 mL	0.4245 mL	0.8490 mL	2.1224 mL
	20 mM	0.0637 mL	0.3184 mL	0.6367 mL	1.5918 mL
	25 mM	0.0509 mL	0.2547 mL	0.5094 mL	1.2734 mL
	30 mM	0.0424 mL	0.2122 mL	0.4245 mL	1.0612 mL
	40 mM	0.0318 mL	0.1592 mL	0.3184 mL	0.7959 mL
	50 mM	0.0255 mL	0.1273 mL	0.2547 mL	0.6367 mL

dBET1 Related Classifications

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:

dBET11799711-21-9dBET 1dBET-1PROTACsEpigenetic Reader DomainInhibitorinhibitorinhibit

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dBET1

Customer Review

Other Forms of dBET1:

dBET1 Related Antibodies

20 Publications Citing Use of MCE dBET1

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PROTACs Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

dBET1 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

dBET1 Related Classifications

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