A NUPR1 inhibitor
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ZZW-115

Item No. 34974

Technical Information
Formal Name
N,N-dimethyl-4-[3-[2-(trifluoromethyl)-10H-phenothiazin-10-yl]propyl]-1-piperazineethanamine, trihydrochloride
CAS Number
10122-45-9
Molecular Formula
C24H31F3N4S • 3HCl
Formula Weight
Purity
≥95%
Formulation
A solid
Ethanol: Soluble
λmax
258 nm
SMILES
FC(F)(C1=CC=C2SC3=C(N(CCCN4CCN(CC4)CCN(C)C)C2=C1)C=CC=C3)F.Cl.Cl.Cl
InChi Code
InChI=1S/C24H31F3N4S.3ClH/c1-28(2)12-13-30-16-14-29(15-17-30)10-5-11-31-20-6-3-4-7-22(20)32-23-9-8-19(18-21(23)31)24(25,26)27;;;/h3-4,6-9,18H,5,10-17H2,1-2H3;3*1H
InChi Key
OBSKIDNFCBBXKJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    ZZW-115 is an inhibitor of nuclear protein 1 (NUPR1).1 It binds to NUPR1 (Kd = 2.1 µM) in a cell-free assay. ZZW-115 is cytotoxic against a panel of 11 pancreatic ductal adenocarcinoma cell lines (IC50s = 0.84-4.93 µM), as well as against a panel of 16 additional cancer cell lines, including glioblastoma, lymphoma, and leukemia cells (IC50s =0.25-7.75 µM). It induces apoptosis and necrosis in MiaPaCa-2, LIPC, Foie8b, 02-063, and HN14 pancreatic cancer cells when used at concentrations of 3 and 5 µM. ZZW-115 induces accumulation of reactive oxygen species (ROS), lipid peroxidation, and ferroptosis in MiaPaCa-2 cells in a concentration-dependent manner.2 It reduces tumor growth in a MiaPaCa-2 mouse xenograft model when administered at doses of 1, 2.5, or 5 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Santofimia-Castaño, P., Xia, Y., Lan, W., et alLigand-based design identifies a potent NUPR1 inhibitor exerting anticancer activity via necroptosis. J. Clin. Invest. 129(6), 2500-2513 (2019).

    2. Huang, C., Santofimia-Castaño, P., Liu, X., et alNUPR1 inhibitor ZZW-115 induces ferroptosis in a mitochondria-dependent manner. Cell Death Discov. 7(1), 269 (2021).