VVD-214

VVD-214 is a synthetic lethal allosteric inhibitor of WRN helicase with an IC50 of 0.1316 µM. VVD-214 covalently binds to cysteine 727 of WRN and inhibits ATP hydrolysis and helicase activity. VVD-214 is potent in causing double-stranded DNA breaks, nuclear swelling, and cell death in high microsatellite instability (MSI) cancers[1][2].

Product Specifications

CAS Number

[3026500-20-6]

Product Name Alternative

RO7589831; VVD-133214

UNSPSC

12352005

Target

DNA/RNA Synthesis

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/vvd-214.html

Concentration

10mM

Purity

99.99

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CS(/C=C/[C@H](C1CC1)NC(C(C(OC2=CC=CC=C2)=N3)=CN=C3C(F)(F)C)=O)(=O)=O

Molecular Formula

C20H21F2N3O4S

Molecular Weight

437.46

References & Citations

[1]Kikuchi S, et al. Abstract ND11: Chemoproteomic-enabled discovery of VVD-214, a synthetic lethal allosteric inhibitor of WRN helicase[J]. Cancer Research, 2024, 84 (7_Supplement) : ND11-ND11.|[2]Kikuchi S, et al., Pharmaceutical compositions comprising wrn helicase inhibitors. WO2024010782.