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Merck

SML3601

ZZW-115 trihydrochloride

≥98% (HPLC)

別名:

10-[3-[4-[2-(Dimethylamino)ethyl]-1-piperazinyl]propyl]-2-(trifluoromethyl)phenothiazine trihydrochloride, N,N-Dimethyl-2-(4-(3-(2-(trifluoromethyl)-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethanamine trihydrochloride, ZZW 115 trihydrochloride, ZZW115 trihydrochloride

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この商品について

実験式(ヒル表記法):
C24H31F3N4S·3HCl
CAS番号:
分子量:
573.97
UNSPSC Code:
12352200
NACRES:
NA.04
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製品名

ZZW-115 trihydrochloride, ≥98% (HPLC)

SMILES string

FC(F)(C1=CC=C2SC3=C(N(CCCN4CCN(CC4)CCN(C)C)C2=C1)C=CC=C3)F.[3HCl]

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

Quality Level

関連するカテゴリー

Biochem/physiol Actions

Nuclear protein 1 (NUPR1) inhibitor that suppresses NUPR1-dependent cancer growth in vitro and in vivo via necroptosis and ferroptosis induction.
ZZW-115 is a nuclear protein 1 (NUPR1) inhibitor that suppresses NUPR1-dependent cancer growth in vitro (IC50 from 0.84 μM/ANOR to 4.93 μM/HN14 among 11 pancreatic ductal adenocarcinoma cultures) and in mice in vivo (5 mg/kg q.d. or q.a.d. via i.p.) via necroptosis and ferroptosis induction. ZZW-115 blocks importins-mediated NUPR1 nuclear translocation by directly targeting NUPR1 nuclear location signal (NLS) region (Kd = 2.1 μM by calorimetric titration).

保管分類

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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Patricia Santofimia-Castaño et al.
The Journal of clinical investigation, 129(6), 2500-2513 (2019-03-29)
Intrinsically disordered proteins (IDPs) are emerging as attractive drug targets by virtue of their prevalence in various diseases including cancer. Drug development targeting IDPs is challenging because they have dynamical structure features and conventional drug design is not applicable. NUPR1
Wenjun Lan et al.
Cancer letters, 486, 8-17 (2020-05-25)
HCC is a highly lethal malignancy with Sorafenib as the only molecularly targeted drug. The multifunctional stress-associated protein, NUPR1, plays an essential role in controlling cell growth, migration, invasion and Sorafenib resistance in HCC. We report here that NUPR1 expression
Patricia Santofimia-Castaño et al.
Cells, 8(11) (2019-11-21)
Cancer cells activate stress-response mechanisms to adapt themselves to a variety of stressful conditions. Among these protective mechanisms, those controlled by the stress-induced nuclear protein 1 (NUPR1 ) belong to the most conserved ones. NUPR1 is an 82-residue-long, monomeric, basic
Jiao Liu et al.
Nature communications, 12(1), 647-647 (2021-01-30)
Ferroptosis is a type of iron-dependent regulated cell death, representing an emerging disease-modulatory mechanism. Transcription factors play multiple roles in ferroptosis, although the key regulator for ferroptosis in iron metabolism remains elusive. Using NanoString technology, we identify NUPR1, a stress-inducible
Wenjun Lan et al.
JCI insight, 5(18) (2020-08-12)
Establishing the interactome of the cancer-associated stress protein Nuclear Protein 1 (NUPR1), we found that it binds to several hundreds of proteins, including proteins involved in nuclear translocation, DNA repair, and key factors of the SUMO pathway. We demonstrated that

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