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SML2233

Sigma-Aldrich

XMU-MP-1 hydrochloride

≥98% (HPLC)

Synonym(s):

4-((5,10-Dimethyl-6-oxo-6,10-dihydro-5H-pyrimido[5,4-b]thieno[3,2-e][1,4]diazepin-2-yl)amino)benzenesulfonamide hydrochloride, 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 hydrochoride

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About This Item

Empirical Formula (Hill Notation):
C17H16N6O3S2 · xHCl
CAS Number:
Molecular Weight:
416.48 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

Pricing and availability is not currently available.

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear (warmed)

storage temp.

−20°C

SMILES string

CN(C1=CN=C(NC2=CC=C(S(N)(=O)=O)C=C2)N=C1N(C)C3=C4SC=C3)C4=O

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1 of 4

This Item
SAB4200783SAB4200790SAB4200713
clone

GG-7, monoclonal

clone

HP-6014, monoclonal

clone

GG-7, monoclonal

clone

GG-5, monoclonal

species reactivity

human

species reactivity

human

species reactivity

human

species reactivity

human

antibody form

purified immunoglobulin

antibody form

purified from hybridoma cell culture

antibody form

purified from hybridoma cell culture

antibody form

purified from hybridoma cell culture

shipped in

dry ice

shipped in

dry ice

shipped in

dry ice

shipped in

dry ice

Quality Level

300

Quality Level

200

Quality Level

200

Quality Level

-

Biochem/physiol Actions

XMU-MP-1 inhibits MST kinase activity (IC50 = 9.8 nM/MST1, 18.2 nM/MST2, 44.8 nM/MST3, 27.3 nM/MST4) in a reversible and ATP-competitive manner (MST1 IC50/[ATP] = 164 nM/10 μM and 4036 nM/300 μM; MST2 IC50/[ATP] = 34 nM/10 μM and 1498 nM/300 μM), exhibiting significant affinity and/or inhibitory potency toward only 17 other kinases among a panel of 468 (401 unique kinases). XMU-MP-1 selectively inhibits H2O2-stimulated MST autophosphorylation and phosphorylation of endogenous MST1/2 substrates (MOB1, LATS, YAP), but not JNK, in human and murine cells (Effective conc. 1 μM), effectively upregulating YAP nuclear localization and protecting HepG2 cells (3 μM) against MST2 overexpression-induced cell death. XMU-MP-1 exhibits in vivo efficacy toward liver and intestinal repair and regeneration in various murine models (1-3 mg/kg/day i.p.) and oral availability in rats (t1/2 = 5.18 h, Tmax = 3 h, AUC = 993 ng•h/mL, F = 39.48%; 10 mg/mL p.o.).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


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