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化驗
≥98% (HPLC)
形狀
solid
顏色
off-white
溶解度
H2O: <2 mg/mL
DMSO: ≥5 mg/mL
儲存溫度
2-8°C
SMILES 字串
NC(=O)c1cccc(c1)-c2cc(Nc3ccc(OC(F)(F)F)cc3)ncn2
InChI
1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25)
InChI 密鑰
WEVYNIUIFUYDGI-UHFFFAOYSA-N
生化／生理作用
GNF-2 belongs to a new class of Bcr-abl inhibitors. GNF-2 appears to bind to the myristoyl binding pocket, an allosteric site distant from the active site, stabilizing the inactive form of the kinase. It inhibits Bcr-abl phosphorylation with an IC50 of 267 nM, but does not inhibit a panel of 63 other kinases, including native c-Abl, and shows complete lack of toxicity towards cells not expressing Bcr-Abl. GNF-2 shows great potential for a new class of inhibitor to study Bcr-abl activity and to treat resistant Chronic myelogenous leukemia (CML), which is caused the Bcr-Abl oncoprotein.
特點和優勢
This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Abl page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
個人防護裝備
dust mask type N95 (US), Eyeshields, Gloves
Melissanne de Wispelaere et al.
Cell chemical biology, 25(8), 1006-1016 (2018-06-26)
Viral envelope proteins are required for productive viral entry and initiation of infection. Although the humoral immune system provides ample evidence for targeting envelope proteins as an antiviral strategy, there are few pharmacological interventions that have this mode of action.
Francisco J Adrián et al.
Nature chemical biology, 2(2), 95-102 (2006-01-18)
Chronic myelogenous leukemia (CML) is a myeloproliferative disorder characterized at the molecular level by the expression of Bcr-abl, a 210-kDa fusion protein with deregulated tyrosine kinase activity. Encouraged by the clinical validation of Bcr-abl as the target for the treatment
Inhibitors of Bcr-abl... breaking new ground again.
Jeffrey F Ohren et al.
Nature chemical biology, 2(2), 63-64 (2006-01-20)
So-Youn Kim et al.
Cell death and differentiation, 26(3), 502-515 (2018-07-11)
Platinum-based chemotherapies can result in ovarian insufficiency by reducing the ovarian reserve, a reduction believed to result from apoptosis of immature oocytes via activation/phosphorylation of TAp63α by multiple kinases including CHEK2, CK1, and ABL1. Here we demonstrate that cisplatin (CDDP)
Yi Luan et al.
Science advances, 8(51), eade1846-eade1846 (2022-12-22)
Cyclophosphamide and doxorubicin lead to premature ovarian insufficiency as an off-target effect. However, their oocyte death pathway has been debated. Here, we clarified the precise mechanism of ovarian depletion induced by cyclophosphamide and doxorubicin. Dormant oocytes instead of activated oocytes
商品
Discover Bioactive Small Molecules for Kinase Phosphatase Biology
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