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SML2233

Sigma-Aldrich

XMU-MP-1 hydrochloride

≥98% (HPLC)

Sinonimo/i:

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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CHF 185.00
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CHF 739.00

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5 MG
CHF 185.00
25 MG
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About This Item

Formula empirica (notazione di Hill):
C17H16N6O3S2 · xHCl
Numero CAS:
2061980-01-4
Peso molecolare:
416.48 (free base basis)
Numero MDL:
MFCD30377214
Codice UNSPSC:
12352200
NACRES:
NA.77

CHF 185.00

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Saggio

≥98% (HPLC)

Stato

powder

Condizioni di stoccaggio

desiccated

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear (warmed)

Temperatura di conservazione

−20°C

Stringa SMILE

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

InChI

1S/C17H16N6O3S2/c1-22-12-7-8-27-14(12)16(24)23(2)13-9-19-17(21-15(13)22)20-10-3-5-11(6-4-10)28(18,25)26/h3-9H,1-2H3,(H2,18,25,26)(H,19,20,21)
YRDHKIFCGOZTGD-UHFFFAOYSA-N

Azioni biochim/fisiol

Potent, reversible, ATP-competitive pan-MST kinase inhibitor with in vivo liver and intestinal tissue repair/regeneration efficacy.
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.).

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

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Masashi Kanayama et al.
Nature immunology, 18(9), 973-984 (2017-07-04)
The balance of myeloid populations and lymphoid populations must be well controlled. Here we found that osteopontin (OPN) skewed this balance during pathogenic conditions such as infection and autoimmunity. Notably, two isoforms of OPN exerted distinct effects in shifting this
Hiroshi Kishimoto et al.
iScience, 26(7), 107146-107146 (2023-07-17)
Non-canonical Wnt signaling activated by Wnt5a/Wnt11 is required for the second heart field development in mice. However, the pathophysiological role of non-canonical Wnt signaling in the adult heart has not been fully elucidated. Here we show that cardiomyocyte-specific Wnt5a knockout
Fuqin Fan et al.
Science translational medicine, 8(352), 352ra108-352ra108 (2016-08-19)
Tissue repair and regenerative medicine address the important medical needs to replace damaged tissue with functional tissue. Most regenerative medicine strategies have focused on delivering biomaterials and cells, yet there is the untapped potential for drug-induced regeneration with good specificity

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