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Merck
CN

SML3601

ZZW-115 trihydrochloride

≥98% (HPLC)

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C24H31F3N4S·3HCl
CAS Number:
Molecular Weight:
573.97
UNSPSC Code:
12352200
NACRES:
NA.04
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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Quality Level

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: 2 mg/mL, clear (Warmed)

storage temp.

2-8°C

SMILES string

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

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).


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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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
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
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



Global Trade Item Number

SKUGTIN
SML3601-10MG04065269337287
SML3601-50MG04065269337294