GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively[1]. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells[2].
IC50 & Target[1]
ADAM17
8 nM (IC50)
ADAM10
11.5 nM (IC50)
体外研究 (In Vitro)
The proliferation of GS-7 cells was significantly reduced upon treatment with GW280264X or ADAM10/17 co-knockdown[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[2]
Cell Line:
Glioblastoma-initiating cells (GIC) GS-7 cells
Concentration:
0.1, 1, and 3 µM
Incubation Time:
48 hours
Result:
Proliferation of GIC is inhibited through inhibition of ADAM10 and ADAM17.
体内研究 (In Vivo)
Pharmacological inhibition of ADAM10 and ADAM17 improves functional recovery after spinal cord injury (SCI)[3].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
C57BL/6 mice[3]
Dosage:
100 µg/kg
Administration:
I.p. injected; every day for one week starting 4 h post-surgery
Result:
Showed significantly improved functional recovery compared to the control group.
分子量
575.72
Formula
C28H41N5O6S
CAS 号
866924-39-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 125 mg/mL (217.12 mM; ultrasonic and warming and heat to 60°C)
[1]. Christian Hundhausen, et al. The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesion. Blood. 2003 Aug 15;102(4):1186-95.
[2]. Fabian Wolpert, et al. A disintegrin and metalloproteinases 10 and 17 modulate the immunogenicity of glioblastoma-initiating cells. Neuro Oncol. 2014 Mar;16(3):382-91.
[3]. Daniela Sommer, et al. ADAM17-deficiency on microglia but not on macrophages promotes phagocytosis and functional recovery after spinal cord injury. Brain Behav Immun. 2019 Aug;80:129-145.