LDN 27219

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Cat.No. 4602 - LDN 27219 | C20H16N4O2S2 | CAS No. 312946-37-5
Description: Transglutaminase 2 (TG2) inhibitor; reversible
Chemical Name: 2-[(3,4-Dihydro-4-oxo-3,5-diphenylthieno[2,3-d]pyrimidin-2-yl)thio]acetic acid hydrazide
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

Transglutaminase 2 (TG2) inhibitor (IC50 = 0.25 μM). Binds at GTPase site; reversible.

Compound Libraries

LDN 27219 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 408.5
Formula C20H16N4O2S2
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 312946-37-5
PubChem ID 1150683
InChI Key WLBUICQBNZXIDJ-UHFFFAOYSA-N
Smiles O=C(NN)CSC(N1C2=CC=CC=C2)=NC3=C(C(C4=CC=CC=C4)=CS3)C1=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.85 100
ethanol 2.04 5mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 408.5. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.45 mL 12.24 mL 24.48 mL
5 mM 0.49 mL 2.45 mL 4.9 mL
10 mM 0.24 mL 1.22 mL 2.45 mL
50 mM 0.05 mL 0.24 mL 0.49 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Case and Stein (2007) Kinetic analysis of the interaction of tissue transglutaminase with a nonpeptidic slow-binding inhibitor. Biochemistry 46 1106 PMID: 17240993

Prime et al (2012) Discovery and structure-activity relationship of potent and selective covalent inhibitors of transglutaminase 2 for Huntington's disease. J.Med.Chem. 55 1021 PMID: 22224594

Duval et al (2005) Structure-activity relationship study of novel tissue transglutaminase inhibitors. Bioorg.Med.Chem.Lett. 15 1885 PMID: 15780627


If you know of a relevant reference for LDN 27219, please let us know.

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View all Other Transferase Inhibitors

Keywords: LDN27219 transglutaminases 2 TG2 TGase tissue tTG inhibits inhibitors reversible Other Transferases

1 Citation for LDN 27219

Citations are publications that use Tocris products. Selected citations for LDN 27219 include:

Yeo et al (2016) Transglutaminase 2 contributes to a TP53-induced autophagy program to prevent oncogenic transformation. Mediators Inflamm 5 PMID: 26956429


Do you know of a great paper that uses LDN 27219 from Tocris? If so please let us know.

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