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.
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
This product is not in stock, which may be available by custom synthesis.
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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 Key: MWRKONWQKZWDTC-VWLOTQADSA-N
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
SMILES Code: O=C(OCC1=CC=CC=C1)N[C@@H](CCCCNC(C=C)=O)C(N2CCN(C(C(C3=O)=CC4=C(O3)C=C(O)C=C4)=O)CC2)=O
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
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.
| 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 |
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.
Patent licensed for this product:
We licensed below patents related to this product for research use:
PCT Int. Appl. (2017), WO 2017179018 A1 20171019.
