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IDH (Isocitrate Dehydrogenase) Inhibitors

IMPDH (Inosine Monosphosphate Dehydrogenase) Inhibitor

MAT2A Inhibitor

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OXPHOS (Mitochondrial Oxidative Phosphorylation of Complex I) Modulator

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Monocarboxylate Transporter 1 (MCT 1) Inhibitor

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Neuroactive/BBB Penetrant

Orexin Receptor Antagonists

SDAM (Serotonin-Dopamine Activity Modulator)

TRK (Tropomyosin Receptor Kinase)(Tyrosine Receptor Kinase) Inhibitor

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CRM1 (exportin 1) Inhibitor(s)

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HCV Protease Inhibitor

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Thymidylate synthase inhibitor

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p53–MDM2 Interaction Inhibitor

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SHP2 Phosphatase Inhibitor

Wip1 Phosphatase Inhibitor

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PARP (Poly (ADP-ribose) polymerase)

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Stem cell research

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NADD8-Activating Enzyme Inhibtor

Proteasome Inhibitor

SUMOylation Inhibitor

Ubiquitin-Activating Enzyme Inhibitor

USP1 (Ubiquitin Specific Protease 1)

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Home > Epigenetics Resch Products > BET Family Protein Degraders > dBET1

dBET1

dBET1 is a potent and selective BRD4 protein degrader. The molecule, dubbed “degronimid”, is harnessed by combining two specific high affinity protein ligands, (+)-JQ1 for BRD4 and Phthalimide for E3 ubiquitin ligase cereblon (CRBN), tethered by a linker. Fully exploiting the cells’ own protein-degrading machinery, the molecule drags the ubiquitin ligase complex into the tagged protein, leading to a fast, sustainable, CRBN-dependent and ligand-guided BRD4 degradation. It is so selective that only three proteins, BRD2, 3, 4, of >7000 within the cell, were affected. dBET1 demonstrated powerful anti-leukemia activities both in cell and in animal model, with few noticeable side effects.

Catalog NO:	CT-DBET1
Synonym:
CAS NO:	1799711-21-9
Mol. Formula:	C38H37ClN8O7S∙0.8H2O
MW:	799.7

** A white powder (picture attached), recrystallized. clean (>99.5% by HPLC) + impeccable 1H-NMR, coming with a quantitative elemental analysis. Bulk Stock!!! Ship within 1 day from Indianapolis.

Pricing and OrderingTechnical Data

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References

NO	Size	Price	In Stock	Quantity
1	5 mg	$100.00	YES
2	10 mg	$150.00	YES
3	50 mg	$450.00	YES
4	100 mg	$750.00	YES

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Solubility : refer to Certificate

Storage : refer to Certificate

Purity : >99.5% (by HPLC at 214 and 254 nm)

Original QC Data : HPLC-MS, NMR, and Quantitative Elemental Analysis

Please Pick Batch NO:

dBET1, lot 02, Certificate of Analysis.pdf
dBET1, lot 02, Appearance (color).pdf

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

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