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Cell Cycle/DNA Damage——p97

p97 (also referred to as VCP) is a highly conserved and abundant AAA+ (ATPases associated with diverse cellular activities) ATPase that plays an essential role in cellular proteostasis. p97 participates in a large number of important cellular activities, including (i) proteasomal degradation, through its roles in extracting proteins from membranes or molecular complexes; (ii) lysosomal degradation via autophagy and endolysosomal sorting; (iii) membrane fusion; and (iv) regulation of intracellular signaling, cell proliferation, and survival. These diverse cellular functions are powered by the chemical energy from ATP hydrolysis and coordinated through the interaction of p97 with as many as 40 cofactors that recruit it to specific subcellular locations and to designated substrates for their remodeling and processing.

Mutations in p97 have been linked to a number of neurodegenerative diseases, and overexpression of wild type p97 is observed in numerous cancers. Furthermore, p97 activity has been shown to be essential for the replication of certain viruses, including poliovirus, herpes simplex virus (HSV), cytomegalovirus (CMV), and influenza. These observations highlight the potential for targeting p97 as a therapeutic approach in neurodegeneration, cancer, and certain infectious diseases.

Cell Cycle/DNA Damage——p97(8)

Cat. No. Product Name CAS No. Purity Chemical Structure
KM3823 CB-5083

CB-5083 是一种首创的,有效的,具有口服活性的,选择性 p97 AAA ATPase/VCP 抑制剂。CB-5083 抑制 p97 AAA ATP 酶结构域 D2,IC50 为 11 nM。

1542705-92-9 99%
KM9691 DBeQ

DBeQ 是一种有效的,选择性的,ATP 竞争性的 p97 抑制剂,对 p97(wt) 和 p97(C522A) 的 IC50 值分别为 1.5 μM 和 1.6 μM,同时可抑制 Vps4IC50 值为 11.5 μM。

177355-84-9 99%
KM10620 Eeyarestatin I

Eeyarestatin I 是一种有效的内质网相关蛋白降解 (ERAD) 抑制剂,是一种有效的蛋白易位抑制剂。Eeyarestatin I 靶向与 p97 相关的去泛素化过程 (PAD),并抑制依赖于 atx3 的去泛素化。Eeyarestatin I 通过促凋亡蛋白 NOXA 诱导细胞死亡,并具有抗癌作用。

412960-54-4 98%
KM11758 ML240

ML240 是一种有效的 p97 抑制剂,抑制 p97 ATPase,IC50 值为 100 nM。

1346527-98-7 99%
KM12236 ML241 hydrochloride

ML241 hydrochloride 是一种有效的 p97 抑制剂,IC50 值为 100 nM。

2070015-13-1 99%
KM5111 MSC1094308

MSC1094308 是一种可逆的、II 型 AAA ATPase (VCP)/p97 和I型 AAA ATPase VPS4B 的变构抑制剂,对VPS4B 和 p97 的IC50 值分别为 0.71 μM 和 7.2 μM。

2219320-08-6 99%
KM7149 NMS-859

NMS-859 是一种有效的,共价的 VCP (p97) 抑制剂,细胞中分别在 60 μM 和 1 mM ATP 的条件下,对野生型 VCP 的 IC50 值分别为 0.37 和 0.36 μM。

1449236-96-7 97%
KM9089 NMS-873

NMS-873 是一种有效,选择性的 VCP/p97 变构抑制剂,IC50 值为 30 nM。

1418013-75-8 99%
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