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1883548-93-3

1883548-93-3 structure
1883548-93-3 structure
  • Name: Mps1-IN-1 dihydrochloride
  • Chemical Name: Mps1-IN-1 dihydrochloride
  • CAS Number: 1883548-93-3
  • Molecular Formula: C28H35Cl2N5O4S
  • Molecular Weight: 608.58
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage Mps1
  • Create Date: 2020-08-08 10:19:19
  • Modify Date: 2024-03-06 12:32:11
  • Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1].

Name Mps1-IN-1 dihydrochloride
Description Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1].
Related Catalog
Target

Mps1:27 nM (Kd)

ALK:21 nM (Kd)

LTK:29 nM (Kd)

PYK2:280 nM (Kd)

FAK:440 nM (IC30)

IGF1R:750 nM (Kd)

INSR:470 nM (Kd)

CLK1:1900 nM (Kd)

ERK2:2900 nM (Kd)

INSRR:1200 nM (Kd)

TNK1:2600 nM (Kd)

TNK2:3100 nM (Kd)

GAK:1100 nM (Kd)

Mps1:367 nM (IC50)

In Vitro Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM. Mps1-IN-1 dihydrochloride also has high affinity for ALK, and LTK, with Kds of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 dihydrochloride (5, 10 μM) induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 dihydrochloride (10 µM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 dihydrochloride (5-10 µM) suppresses the proliferative capacity of HCT116[1].
References

[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.

Molecular Formula C28H35Cl2N5O4S
Molecular Weight 608.58