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MS 6105

Cat. No. 8073 Submit a Review Datasheet / COA / SDS
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Description: Potent lactate dehydrogenase Degrader (PROTAC®)
Chemical Name: 2-(5-(Cyclopropylmethyl)-3-(3-(6-(13-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-13-oxotridecanamido)hex-1-yn-1-yl)phenyl)-4-(4-sulfamoylbenzyl)-1H-pyrazol-1-yl)thiazole-4-carboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MS 6105

MS 6105 is a potent and selective lactate dehydrogenase (LDH) Degrader (PROTAC®; for LDHA and LDHB respectively, DC50 values are 38 nM and 74 nM; Dmax is 93% and 86%). Comprises an LDH inhibitor warhead connected by a linker to a VHL ligand. Suppresses growth of several pancreatic cancer cell lines (IC50 range is 12.2 μM - 16.1 μM). Bioavailable in vivo.

Technical Data for MS 6105

M. Wt 1228.6
Formula C65H81N9O9S3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2891709-58-1
PubChem ID 166642429
InChI Key APEYSKGQWJKJAZ-LCLGPXMOSA-N
Smiles O=C([C@@H](NC(CCCCCCCCCCCC(NCCCCC#CC1=CC=CC(C2=NN(C(CC3CC3)=C2CC4=CC=C(S(N)(=O)=O)C=C4)C5=NC(C(O)=O)=CS5)=C1)=O)=O)C(C)(C)C)N6[C@H](C(NCC7=CC=C(C=C7)C8=C(C)N=CS8)=O)C[C@@H](O)C6

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for MS 6105

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 122.86 100

Preparing Stock Solutions for MS 6105

The following data is based on the product molecular weight 1228.6. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.81 mL 4.07 mL 8.14 mL
5 mM 0.16 mL 0.81 mL 1.63 mL
10 mM 0.08 mL 0.41 mL 0.81 mL
50 mM 0.02 mL 0.08 mL 0.16 mL

Molarity Calculator

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References for MS 6105

References are publications that support the biological activity of the product.

Sun et al (2023) Discovery of the first lactate dehydrogenase proteolysis targeting chimera degrader for the treatment of pancreatic cancer. J.Med.Chem. 66 596 PMID: 36538511

If you know of a relevant reference for MS 6105, please let us know.

View Related Products by Target

Keywords: MS 6105, MS 6105 supplier, MS6105, lactate, dehydrogenase, LDHA, degrader, degrades, degraders, proteolysis, targeting, chimera, PROTAC, VHL, von, hippel, lindau, E3, ligase, proteosome, Other, Degraders, 8073, Tocris Bioscience

Citations for MS 6105

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia