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经验公式(希尔记法):
C25H23N5O2S
化学文摘社编号:
分子量:
457.55
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
SMILES string
[s]1c2c(nc1C(c3nc(ncc3)OCc4ccc(cc4)CN5CCOCC5)C#N)cccc2
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear (Warmed)
storage temp.
2-8°C
Quality Level
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).
Orally active, ATP-competitive, potent and selective c-Jun N-terminal kinase (JNK) inhibitor in vitro and in vivo.
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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
Jonas Cicenas et al.
Cancers, 10(1) (2017-12-22)
Mitogen-activated protein kinases (MAP kinases) are a family of kinases that regulates a range of biological processes implicated in the response to growth factors like latelet-derived growth factor (PDGF), epidermal growth factor (EGF), vascular endothelial growth factor (VEGF), and stress
Shuai Zhang et al.
Journal of cellular and molecular medicine, 25(8), 4062-4072 (2021-02-21)
Previous studies showed that the chemotherapeutic effect of temozolomide (TMZ) and vincristine (VCR) against glioma might be blunted by the co-culture with astrocytes, and connexin-43 (CX43) was thought to play a vital role in the communication between glioma cells and
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, 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
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