BiochemProbe — Life Science Research Reagents

VVD-214 free base · Synonyms: VVD-133214 | RO7589831

VVD-133214 is a covalent allosteric inhibitor of WRN.

For research use only. Not for human or veterinary use.

Research area Cancer
Purity >98% Stock Inquire

VVD-214 structure

CAS No.: 3026500-20-6

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
100 mg USD 480.00 BP-00122-100mg In stock Get quote
250 mg USD 780.00 BP-00122-250mg In stock Get quote
500 mg USD 1,180.00 BP-00122-500mg In stock Get quote
1 g USD 1,680.00 BP-00122-1g In stock Get quote
5 g Inquire BP-00122-5g Inquire Inquire

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Description

VVD-133214 is a covalent allosteric inhibitor of WRN. It selectively engages a cysteine (C727). VVD-133214 binds WRN protein cooperatively with nucleotide. VVD-133214 can be used for MSI-H cancers study.

Biological activity

VVD-214 is a synthetic lethal allosteric inhibitor of WRN helicase. 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.

Specifications

MW (average)
437.4600
Formula
C20H21F2N3O4S
CAS No.
3026500-20-6
Physical state
Solid
Color
White to off-white
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

References

[1]. Baltgalvis KA, Lamb KN, Symons KT, et al. Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase. Nature. Published online April 24, 2024. doi:10.1038/s41586-024-07318-y
[2]. 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.

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