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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

Curated Selection

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