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dBET1

  Cat. No.:  DC12023   Featured
Chemical Structure
1799711-21-9
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More than 5000 active chemicals with high quality for research!
Field of application
dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1799711-21-9
Chemical Name: 2-[(6s)-4-(4-Chlorophenyl)-2,3,9-Trimethyl-6h-Thieno[3,2-F][1,2,4]triazolo[4,3-A][1,4]diazepin-6-Yl]-N-(4-{[({2-[(3s)-2,6-Dioxopiperidin-3-Yl]-1,3-Dioxo-2,3-Dihydro-1h-Isoindol-4-Yl}oxy)acetyl]amino}butyl)acetamide
Synonyms: 2-[(6s)-4-(4-Chlorophenyl)-2,3,9-Trimethyl-6h-Thieno[3,2-F][1,2,4]triazolo[4,3-A][1,4]diazepin-6-Yl]-N-(4-{[({2-[(3s)-2,6-Dioxopiperidin-3-Yl]-1,3-Dioxo-2,3-Dihydro-1h-Isoindol-4-Yl}oxy)acetyl]amino}butyl)acetamide;A16858;4MW;dBET1
SMILES: ClC1C([H])=C([H])C(=C([H])C=1[H])C1C2C(C([H])([H])[H])=C(C([H])([H])[H])SC=2N2C(C([H])([H])[H])=NN=C2[C@]([H])(C([H])([H])C(N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(C([H])([H])OC2=C([H])C([H])=C([H])C3=C2C(N(C3=O)[C@]2([H])C(N([H])C(C([H]
Formula: C38H37ClN8O7S
M.Wt: 785.2678
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
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].
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].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC55003 XY028-140 (MS140) XY028-140 (MS-140) is a potent and selective PROTAC-based CDK4/CDK6 kinase degrader. XY028-140 specifically inhibits RB-E2F signaling and reduces CDK4 and CDK6 protein levels in a dose- and time-dependent manner in vitro. In addition, XY028-140 can degrade its targets by linking them with ubiquitin-proteasome mechanism. Further, the degradation of CDK4/6 protein by XY028-140 is specifically mediated by CRBN. Therefore, XY028-140 effectively and selectively inhibits and degrades CDK4/6 kinase by targeting CDK4/6 kinase in CDK4/6i-S (CDK4/6 inhibitor-sensitive) tumor cells to the CRL4-CRBN-E3 ubiquitin complex. Compared with CDK6 wild-type cells, XY028-140 treatment of cells expressing wild-type or mutation-activated CDK6 resulted in a more effective degradation of CDK6 (S178P).
DC53120 XD2-149 XD2-149 is a napabucasin PROTAC as an effective degrader of the E3 ligase ZFP91 with IC50 of 1 μM and 0.8 μM in pancreatic cancer cell lines, MIA PaCa-2 and BxPC-3, respectively. XD2-149 also reduces the expression of STAT3, pSTAT3, and NQO1 proteins.
DC51010 CID 138454799 ERD-308 is a highly potent PROTAC degrader of estrogen receptor (ER) for ER positive breast cancer treatment.
DC31014 GMB-475 GMB-475 is a degrader of BCR-ABL1 tyrosine kinase based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein[1].
DC28018 MD-224 MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
DC12022 dBET6 dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity.
DC12023 dBET1 dBET1 is a potent BRD4 protein degrader based on PROTAC technology with an EC50 of 430 nM.
DC12380 BSJ-03-123 BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC) that uniquely enables rapid pharmacological interrogation of CDK6-dependent functions.
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