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Key Documents

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SML3358

Sigma-Aldrich

AS602801

≥98% (HPLC)

Sinónimos:

1,3-Benzothiazol-2-yl(2-{[4-(morpholin-4-ylmethyl)benzyl]oxy}pyrimidin-4-yl)-acetonitrile, 2-(Benzo[d]thiazol-2-yl)-2-(2-(4-(morpholinomethyl)benzyloxy)pyrimidin-4-yl)acetonitrile, AS 602801, AS-602801, Bentamapimod, PGL 5001, PGL-5001, PGL5001

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About This Item

Fórmula empírica (notación de Hill):
C25H23N5O2S
Número de CAS:
848344-36-5
Peso molecular:
457.55
MDL number:
MFCD08272350
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

InChI

1S/C25H23N5O2S/c26-15-20(24-28-22-3-1-2-4-23(22)33-24)21-9-10-27-25(29-21)32-17-19-7-5-18(6-8-19)16-30-11-13-31-14-12-30/h1-10,20H,11-14,16-17H2

InChI key

XCPPIJCBCWUBNT-UHFFFAOYSA-N

Biochem/physiol Actions

AS602801 (Bentamapimod, PGL5001) is an orally active, ATP-competitive, potent and selective c-Jun N-terminal kinase (JNK) inhibitor (JNK1/2/3 IC50 = 80/90/230 nM). AS602801 decreases MMP-3 upregulation in endometrium cultures from patients with endometriosis (15 μM alone or 5 μM in combination with 100-250 μM medroxyprogesterone acetate) and exhibits therapeutic efficacy in rodent endometriosis models in vivo (10-30 mg/kg via daily p.o. in mice and 10-60 mg/kg via twice daily p.o. in rats).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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Stephen S Palmer et al.
Reproductive sciences (Thousand Oaks, Calif.), 23(1), 11-23 (2015-09-04)
Endometriosis is an estrogen (ER)-dependent gynecological disease caused by the growth of endometrial tissue at extrauterine sites. Current endocrine therapies address the estrogenic aspect of disease and offer some relief from pain but are associated with significant side effects. Immune
Masahiro Yamamoto et al.
Anticancer research, 38(12), 6699-6706 (2018-12-07)
AS602801, a novel inhibitor of c-Jun N-terminal kinase (JNK), suppresses tumor initiation capacity and metastatic potential of cancer stem cells (CSCs). However, it remains unknown whether this inhibitor can chemosensitize CSCs. Using A2780 CSLC, a CSC line derived from ovarian
Maohua Chen et al.
Oncotarget, 7(45), 73903-73911 (2016-09-23)
Notch signaling is a highly conserved pathway that regulates cell fate decisions during embryonic development. Notch activation endangers neurons by modulating NF-κB and HIF-1α pathways, however, the role of Notch signaling in activating JNK/c-Jun following intracerebral hemorrhage (ICH) has not
Masahiro Yamamoto et al.
Anticancer research, 39(2), 609-617 (2019-02-04)
AS602801, an anti-cancer stem cell (CSC) candidate drug, sensitizes ovarian CSCs to paclitaxel and carboplatin by reducing the expression of survivin, an anti-apoptotic protein. The aim of the study was to examine the effect of AS602801 on the expression of
Zhenghong Li et al.
Translational oncology, 13(4), 100751-100751 (2020-03-22)
In our previous study, we observed that androgen deprivation therapy (ADT) may induce a compensatory increase in MAPK or JNK signaling. Here, we tested the effects of the MEK inhibitors PD0325901 and GSK1120212, ERK1/2 inhibitor GDC-0994, and the JNK inhibitor

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