XMU MP 1

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Cat.No. 6482 - XMU MP 1 | C17H16N6O3S2 | CAS No. 2061980-01-4
Description: Potent and selective MST1/2 inhibitor; orally bioavailable
Chemical Name: 4-[(6,10-Dihydro-5,10-dimethyl-6-oxo-5H-pyrimido[5,4-b]thieno[3,2-e][1,4]diazepin-2-yl)amino]benzenesulfonamide
Purity: ≥98% (HPLC)
Datasheet
Citations
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Literature

Biological Activity

Potent and selective ATP-competitive mammalian sterile 20-like kinase (MST) 1/2 inhibitor (IC50 values are 38.1 and 71.1 nM for MST2 and MST1, respectively). Enhances activity of downstream YAP in vitro. Augments mouse intestinal repair and promotes liver repair and regeneration in a mouse model of acute and chronic liver injury. Orally bioavailable.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data

M. Wt 416.48
Formula C17H16N6O3S2
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2061980-01-4
PubChem ID 121499143
InChI Key YRDHKIFCGOZTGD-UHFFFAOYSA-N
Smiles CN1C2=C(C(N(C3=CN=C(N=C13)NC4=CC=C(S(N)(=O)=O)C=C4)C)=O)SC=C2

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.65 100

Preparing Stock Solutions

The following data is based on the product molecular weight 416.48. 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.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.4 mL 12.01 mL 24.01 mL
5 mM 0.48 mL 2.4 mL 4.8 mL
10 mM 0.24 mL 1.2 mL 2.4 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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References

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

Fan et al (2016) Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration. Sci.Transl.Med. 8 352 PMID: 27535619

Ray et al (2016) Therapy: Targeting liver tissue repair and regeneration. Nat.Rev.Gastroenterol.Hepatol. 13 559 PMID: 27605063

Crunkhorn et al (2016) Regenerative medicine: Inhibiting Hippo repairs tissue. Nat.Rev.Drug Discov. 15 678 PMID: 27681796


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