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Datasheet of Necrostatin-1

Description:
Necrostatin-1 is a specific RIP1 inhibitor and inhibits TNF--induced necroptosis with EC50 of 490 nM.
Necrostatin-1 is an inhibitor of necroptosis, a mechanism of programmed cell death separate from apoptosis. Necrostatin-1
functions as an allosteric inhibitor of the death domain receptor-associated adaptor kinase RIP (RIP1) in the necroptosis pathway.
While affecting this distinct cell death pathway, Necrostatin-1 does not present any perturbation of the Fas/TNFR triggered
canonical apoptosis cascade.
in vitro: Shikonin-induced necroptosis can be reverted to apoptosis in the presence of necrostatin-1 (Nec-1), a specific
necroptosis inhibitor and that the death mode switch is at least partially due to the conversion from mitochondrial inner
membrane permeability to mitochondrial outer membrane permeability, which is associated with Bax translocation. The cell
viabilities inhibited by Al could be enhanced by 3-MA, zVAD-fmk and Nec-1, of which Nec-1 improved the cell viability most
significantly. Furthermore, the cell viability of neural cells treated with Nec-1 increased concentration-dependently, and the
expressions of cell death-related proteins were decreased also in a concentration-dependent manner .
in vivo: In a mouse model of myocardial infarction, survival of CMPCs 3 days after intra-myocardial injection was 39 9%
higher in cells pretreated with the Nec-1 compound. However, the increase in cell number was not sustained over 28 days, and
did not translate into improved cardiac function (ejection fraction %, 20.6 2.1 vs. 21.4 2.5 for vehicle and Nec-1-treated
CMPC, respectively). Mice pretreated with NEC-1 reduced the amount of PI-positive cells from 12 to 48 h after TBI.
Immunoblotting results showed that NEC-1 suppressed TBI-induced Beclin-1 and LC3-II activation which maintained p62 at
high level. NEC-1 pretreatment also reversed TBI-induced Bcl-2 expression and caspase-3 activation, as well as the ratio of
Beclin-1/Bcl-2. Both 3-MA and NEC-1 suppressed TBI-induced caspase-3 activation and LC3-II formation, Z-VAD only
inhibited caspase-3 activation but increased LC3-II expression at 24 h post-TBI.

Chemical Information
Catalog

DC2084

Purity of current batch:

>98%

Molecular Weight (MW)

259.33

Molecular Formula

C13H13N3OS

CAS No.

4311-88-0

Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.