2. PROTAC Epigenetics
  3. PROTACs Epigenetic Reader Domain
  4. CFT-743

CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research.

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

CFT-743

CFT-743 Chemical Structure

CAS No. : 2154350-81-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

CFT-743 Related Antibodies

Top Publications Citing Use of Products

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CFT-743, a PROTAC-based heterobifunctional degrader and BET inhibtor, is a degrader of BRD4 bromodomain 1 (BD1) with a DC50 of 4.3 nM. CFT-743's antitumor activitiy is dependent on BET degradation and can be attenuated by Pomalidomide (HY-10984), which is a CRBN binding molecule. CFT-743 induces ubiquitination of BRD4 BD1. CFT-743 can be used for cancer research[1][2].

IC50 & Target[1]

BRD4

4.3 nM (DC50)

In Vitro

CFT-743 binds tightly to both purified BRD4 BD1 and purified CRBN-DDB1 complex, with minimal cooperative effects between the two proteins during ternary complex formation[1].
CFT-743 drives ternary complex formation between purified BRD4 BD1 and purified CRBN-DDB1 with high affinity, and exhibits minimal protein-protein cooperativity in this complex[1].
CFT-743 (3-1000 nM; 30-90 min) induces low-rate ubiquitination of purified HA-tagged BRD4 BD1 in HeLa cell-free lysates, with tight binding to BD1 and moderate binding to CRBN, following an essential activator kinetic model[1].
CFT-743 (10 µM down to serially diluted half-log concentrations; 3 h) induces minimal degradation of HiBiT-tagged BRD4 BD1 in 293T cells, with a DC50 of 4.3 nM and very low maximal efficacy[1].
CFT-743 (30-3000 nM; 30-90 min) induces low-rate ubiquitination of endogenous BRD4 in HeLa cell-free lysates, with a slower maximal velocity compared to purified BRD4 BD1 due to lower endogenous target concentration[1].
CFT-743 preferentially induces diubiquitination of purified HA-tagged BRD4 BD1 in HeLa cell-free lysates, unlike other tested BiDACs that predominantly induce monoubiquitination[1].

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

CFT-743 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 (Plasma) Tmax (Plasma) Cmax (Brain) AUC0-∞ (Plasma) AUC0-∞ (Brain)
Mice[2] 10 mg/kg p.o. 3.7 h 0.5 h 2990 ng/g 63100 ng·h/mL 9910 h·ng/g
Mice[2] 10 mg/kg p.o. 3.7 h 0.5 h 2990 ng/g 63100 ng·h/mL 9910 h·ng/g
Molecular Weight

825.40

Formula

C46H49ClN10O3
CAS No.
SMILES

O=C1C2=C(CN1C3C(NC(CC3)=O)=O)C(NC4CCN(CC4)CCCCCCN5N=CC(C6=CC=C7C(C(C8=CC=C(C=C8)Cl)=NC9(CC9)C%10=NN=C(C)N7%10)=C6)=C5)=CC=C2
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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

CFT-743 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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:

CFT-7432154350-81-7CFT743CFT 743PROTACsEpigenetic Reader DomainPROTACCRBNBRD4 bromodomain 1diubiquitinationcereblon293T cellsternary complexHeLa cell-free lysatesubiquitinationmonoubiquitinationBRD4 BD1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CFT-743
Cat. No.:
HY-182577
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.