PLX-3618
PLX-3618 is a molecular glue, that degrades BRD4 with DC50 of 12.2 nM. PLX-3618 promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting of the E3 ligase substrate receptor, DCAF11. PLX-3618 inhibits the proliferation of various cancer cells, induces apoptosis in AML cells. PLX-3618 exhibits antitumor activity against AML in mouse models[1].
Product Specifications
CAS Number
2851986-76-8
UNSPSC
12352005
Target
Apoptosis; Epigenetic Reader Domain; Molecular Glues
Type
Reference compound
Related Pathways
Apoptosis; Epigenetics; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/plx-3618.html
Concentration
10mM
Purity
99.86
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(C5=CC=CC(NC(C6=C7N(C=CC=N7)N=C6)=O)=C5)C=C4)=N1
Molecular Formula
C32H27N9O2S
Molecular Weight
601.68
References & Citations
[1]Parker GS, et al., Discovery of Monovalent Direct Degraders of BRD4 That Act Via the Recruitment of DCAF11. Mol Cancer Ther. 2024 Jun 22.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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