VA5 TG2 inhibitor

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561184

CAS#: 2088001-24-3

Description: VA5 inhibits both transamidase and GTP-binding activities. Transamidase activity is inhibited by direct inhibitor binding at the transamidase site, and GTP binding is blocked because inhibitor interaction at the transamidase site locks the protein in the extended/open conformation to disorganize/inactivate the GTP binding/GTPase site.

Chemical Structure

VA5 TG2 inhibitor
CAS# 2088001-24-3

Theoretical Analysis

MedKoo Cat#: 561184
Name: VA5 TG2 inhibitor
CAS#: 2088001-24-3
Chemical Formula: C31H34N4O8
Exact Mass: 590.2377
Molecular Weight: 590.633
Elemental Analysis: C, 63.04; H, 5.80; N, 9.49; O, 21.67

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: VA5; VA-5; VA 5; VA5 TG2 inhibitor

IUPAC/Chemical Name: (S)-Benzyl (6-acrylamido-1-(4-(7-hydroxy-2-oxo-2H-chromene-3-carbonyl)piperazin-1-yl)-1-oxohexan-2-yl)carbamate


InChi Code: InChI=1S/C31H34N4O8/c1-2-27(37)32-13-7-6-10-25(33-31(41)42-20-21-8-4-3-5-9-21)29(39)35-16-14-34(15-17-35)28(38)24-18-22-11-12-23(36)19-26(22)43-30(24)40/h2-5,8-9,11-12,18-19,25,36H,1,6-7,10,13-17,20H2,(H,32,37)(H,33,41)/t25-/m0/s1


Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 590.633 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Kerr C, Szmacinski H, Fisher ML, Nance B, Lakowicz JR, Akbar A, Keillor JW, Lok Wong T, Godoy-Ruiz R, Toth EA, Weber DJ, Eckert RL. Transamidase site-targeted agents alter the conformation of the transglutaminase cancer stem cell survival protein to reduce GTP binding activity and cancer stem cell
survival. Oncogene. 2017 May 25;36(21):2981-2990. doi: 10.1038/onc.2016.452. Epub 2016 Dec 12. PubMed PMID: 27941875; PubMed Central PMCID: PMC5444990.

Additional Information

Patent licensed for this product:
We licensed below patents related to this product for research use:
PCT Int. Appl. (2017), WO 2017179018 A1 20171019.