BML-284 - CAS 853220-52-7
Catalog number: B0084-474867
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C19H18N4O3
Molecular Weight:
350.37
COA:
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Targets:
Wnt
Description:
BML-284 is potent selective, and cell-permeable Wnt signaling activator that does not inhibit GSK-3β (IC50 > 60 µM). It appears to mimic the effects of a Wnt ligand in a Xenopus model and may be a useful tool in the study of physiological processes that involve the Wnt pathway in vivio. It is effective in vivo, decreasing tissue damage and improving renal function after ischemia-reperfusion in rats. It induces in vitro β-catenin and transcription factor (TCF) dependent transcriptional activity in 293T cells in a dose dependent manner with an EC50 of 0.7 mM in vitro.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-474867 25 mg $198 In stock
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Purity:
>98%
Appearance:
Solid powder
Synonyms:
AMBMP HCl; AMBMP Hydrochloride; BML284 HCl; Wnt Agonist; BML284 HCl; BML-284 HCl; BML 284 HCl; Wnt Agonist;IN1013;2-Amino-4-(3,4-(methylenedioxy)benzylamino)-6-(3-methoxyphenyl)pyrimidine;4-N-(1,3-benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)pyrimidine-2,4-diamine;N4-(1,3-benzodioxol-5-ylmethyl)-6-(3-methoxyphenyl)-2,4-pyrimidinediamine
Solubility:
DMSO: ≥ 30 mg/mL
Storage:
2-8°C
MSDS:
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Application:
BML-284 may be a useful tool in the study of physiological processes that involve the Wnt pathway.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams-Kilos
Boiling Point:
623.4±65.0 °C | Condition: Press: 760 Torr
Density:
1.353±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
FABQUVYDAXWUQP-UHFFFAOYSA-N
InChI:
InChI=1S/C19H18N4O3/c1-24-14-4-2-3-13(8-14)15-9-18(23-19(20)22-15)21-10-12-5-6-16-17(7-12)26-11-25-16/h2-9H,10-11H2,1H3,(H3,20,21,22,23)
Canonical SMILES:
COC1=CC=CC(=C1)C2=CC(=NC(=N2)N)NCC3=CC4=C(C=C3)OCO4
1.2-Amino-4-(3,4-(methylenedioxy)benzylamino)-6-(3-methoxyphenyl)pyrimidine is an anti-inflammatory TLR-2, -4 and -5 response mediator in human monocytes.
Wang H;Graves MW 2nd;Zhou H;Gu Z;Lamont RJ;Scott DA Inflamm Res. 2016 Jan;65(1):61-9. doi: 10.1007/s00011-015-0891-0. Epub 2015 Nov 27.
OBJECTIVE AND DESIGN: ;To elucidate the influence of 2-amino-4-(3,4-(methylenedioxy)benzylamino)-6-(3-methoxyphenyl)pyrimidine (AMBMP), a canonical Wnt/β-catenin pathway activator, on the inflammatory response of TLR-engaged innate cells in vitro.;MATERIAL OR SUBJECT: ;Primary human monocytes.;TREATMENT: ;AMPMB (0-10 μM), LPS (0-1.0 μg/ml), Pam3CSK4, FSL-1, or S. typhimurium flagellin (0-0.25 μg/ml).;METHODS: ;TLR-induced cytokine release (TNF, IL-6, IL-12 p40) was monitored by ELISA while Wnt-related signals (GSK3β, p65, IκB, β-catenin) were assessed by Western blot, pharmaceutical inhibition and gene silencing.;RESULTS: ;AMBMP induced the rapid phosphorylation of NFκB p65 at Ser(536) and abrogated total IκB, accompanied by a subsequent increase in pro-inflammatory cytokine production (TNF, IL-6, IL-12 p40) in otherwise naive monocytes. However, in TLR2, -4 and -5-engaged monocytes, AMBMP-suppressed cytokine production. In the context of LPS stimulation, this occurred concomitant with the phosphorylative inactivation of GSK3β at Ser(9), β-catenin accumulation and abrogation of NFκB p65 phosphorylation. AMBMP-mediated suppression of the TLR4 -induced inflammatory response was reversed by two pharmaceutical Wnt/β-catenin pathway inhibitors, IWP-2 and PNU-74654 and by Wnt3a silencing.
2.Activation of beta-catenin signalling by GSK-3 inhibition increases p-glycoprotein expression in brain endothelial cells.
Lim JC;Kania KD;Wijesuriya H;Chawla S;Sethi JK;Pulaski L;Romero IA;Couraud PO;Weksler BB;Hladky SB;Barrand MA J Neurochem. 2008 Aug;106(4):1855-65. doi: 10.1111/j.1471-4159.2008.05537.x. Epub 2008 Jul 4.
This study investigates involvement of beta-catenin signalling in regulation of p-glycoprotein (p-gp) expression in endothelial cells derived from brain vasculature. Pharmacological interventions that enhance or that block beta-catenin signalling were applied to primary rat brain endothelial cells and to immortalized human brain endothelial cells, hCMEC/D3, nuclear translocation of beta-catenin being determined by immunocytochemistry and by western blot analysis to confirm effectiveness of the manipulations. Using the specific glycogen synthase kinase-3 (GSK-3) inhibitor 6-bromoindirubin-3'-oxime enhanced beta-catenin and increased p-gp expression including activating the MDR1 promoter. These increases were accompanied by increases in p-gp-mediated efflux capability as observed from alterations in intracellular fluorescent calcein accumulation detected by flow cytometry. Similar increases in p-gp expression were noted with other GSK-3 inhibitors, i.e. 1-azakenpaullone or LiCl. Application of Wnt agonist [2-amino-4-(3,4-(methylenedioxy) benzylamino)-6-(3-methoxyphenyl)pyrimidine] also enhanced beta-catenin and increased transcript and protein levels of p-gp. By contrast, down-regulating the pathway using Dickkopf-1 or quercetin decreased p-gp expression.
3.Wnt agonist stimulates liver regeneration after small-for-size liver transplantation in rats.
Ma Y;Lv X;He J;Liu T;Wen S;Wang L Hepatol Res. 2016 Mar;46(3):E154-64. doi: 10.1111/hepr.12553. Epub 2015 Aug 4.
AIM: ;Liver regeneration is inhibited in small-for-size grafts, which plays a role in the failure of partial liver grafts after transplantation. The Wnt/β-catenin signaling pathway plays a critical role in liver development, regeneration and homeostasis. In this study, we investigated whether pharmacological activation of Wnt signaling improves liver regeneration after small-for-size liver transplantation.;METHODS: ;The livers of male Sprague-Dawley rats were reduced to approximately 50% and 30% of their original sizes and transplanted. A Wnt agonist (2-amino-4-[3,4-[methylenedioxy]benzylamino]-6-[3-methoxyphenyl] pyrimidine], 5 mg/kg bodyweight) or an equal volume of vehicle was administrated i.p. into the donor 1 h before the transplantation. Tissue and blood samples were collected at various times after transplantation, and a survival study was performed.;RESULTS: ;Hepatic expression of active β-catenin and its downstream target gene Axin2 were decreased in 30% of liver grafts after transplantation while the Wnt agonist increased their expression similar to the 50% liver grafts. The Wnt agonist reversed inhibition of cyclin D1 expression and adenosine triphosphate production in the 30% liver grafts compared with the 50% grafts.
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CAS 853220-52-7 BML-284

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