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Cat. No. M9237
dBET1 Structure
Size Price Availability Quantity
5mg USD 158 In stock
10mg USD 278 In stock
25mg USD 588 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

dBET1 treatment down regulates MYC and PIM1 transcription. 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).

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 785.27
Formula C38H37ClN8O7S
CAS Number 1799711-21-9
Purity >98%
Solubility DMSO 40 mg/mL
Storage at -20°C

Phthalimide conjugation as a strategy for in vivo target protein degradation.
Winter GE, et al. Science. 2015 Jun 19;348(6241):1376-81. PMID: 25999370.

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Keywords: dBET1 supplier, Epigenetic Reader Domain, inhibitors

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