| Bioactivity | KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than for other MMPs and ADAM10, and IC50s are 11.1 nM (ADAM17), 748 nM (ADAM10), 717 nM (MMP2), 9760 nM (MMP3), 2200 nM (MMP8), 5410 nM (MMP9), 930 nM (MMP13), 2140 nM (MMP14), and 7100 nM (MMP17), respectively. | ||||||||||||
| Invitro | KP-457 是一种选择性金属蛋白酶 17 (ADAM17) 抑制剂，对 ADAM17 的选择性高于对其他 MMP 和 ADAM10 的选择性，IC50 分别为 11.1 nM (ADAM17)、748 nM (ADAM10)、717 nM (MMP2)、9760 nM (MMP3))、2200 nM (MMP8)、5410 nM (MMP9)、930 nM (MMP13)、2140 nM (MMP14) 和 7100 nM (MMP17)。KP-457 阻断 ADAM17 催化结构域的 Zn2+ 螯合。KP-457 (15 μM) 在 iPSC 衍生的血小板上保留 GPIbα 的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> KP-457 相关抗体: | ||||||||||||
| In Vivo | 在使用血小板输注后免疫缺陷小鼠的血栓形成模型中，使用 KP-457 生成的诱导多能干细胞 (iPSC) 血小板具有良好的止血功能[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. | ||||||||||||
| CAS | 1365803-52-6 | ||||||||||||
| Formula | C21H24N2O7S2 | ||||||||||||
| Molar Mass | 480.55 | ||||||||||||
| Appearance | 固体 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Hirata S, et al. Selective Inhibition of ADAM17 Efficiently Mediates Glycoprotein Ibα Retention During Ex Vivo Generation of Human Induced Pluripotent Stem Cell-Derived Platelets. Stem Cells Transl Med. 2017 Mar;6(3):720-730. |
KP-457
CAS: 1365803-52-6 F: C21H24N2O7S2 W: 480.55
KP-457 is a selective a disintegrin and metalloproteinase 17 (ADAM17) inhibitor, with higher selectivity for ADAM17 than
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