Free shipping on all orders over $ 500

SM-164

Cat. No. M6187
SM-164 Structure
Size Price Availability Quantity
5mg USD 360 In stock
10mg USD 560 In stock
50mg USD 1770 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: SM-164 induced complete cIAP-1 degradation, it displayed weak inhibitory effects on the viability of HCC cells. Nevertheless, SM-164 considerably potentiated Apo2 ligand or TNF-related apoptosis-inducing ligand (APO2L/TRAIL)- and Doxorubicin-mediated anticancer activity in HCC cells. Mechanistic studies demonstrated that SM-164 in combination with chemotherapeutic agents resulted in enhanced activation of caspases-9, -3 and cleavage of poly ADP-ribose polymerase (PARP), and also led to decreased AKT activation. Although SM-164 is modestly more effective than SM-122 in induction of cIAP-1/2 degradation, SM-164 is 1,000 times more potent than SM-122 as an inducer of apoptosis in tumor cells, which is attributed to its much higher potency in binding to and antagonizing XIAP. SM-164 radiosensitization in sensitive cells was associated with NF-κB activation and TNFα secretion, followed by activation of caspase-8 and -9, leading to enhanced apoptosis.

In vivo: SM-164 induces rapid cIAP-1 degradation and strong apoptosis in the MDA-MB-231 xenograft tumor tissues and achieves tumor regression, but has no toxicity in normal mouse tissues. SM-164 also radiosensitized human tumor xenograft while causing minimal toxicity.

Protocol
Cell Experiment
Cell lines Breast cancer lines, including SK-BR-3, MDA-MB-468, MDA-MB-453, MCF-7, ZR-75-1, T-47D
Preparation method Cell were seeded in 96-well plates in triplicate and treated the next day with SM-164 in various doses ranging from 0.03 to 10 μM for 24 h. The viability of the cells was then measured using one-step ATPlite cell proliferation assay.
Concentrations 0.03 to 10 μM
Incubation time 24 h
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 1121.42
Formula C62H84N14O6
CAS Number 957135-43-2
Purity >98%
Solubility 10 mM in DMSO
Storage at -20°C
References

Smac mimetic SM-164 potentiates APO2L/TRAIL- and doxorubicin-mediated anticancer activity in human hepatocellular carcinoma cells.
Zhang S, et al. PLoS One 2012;7(12):e51461. PMID: 23240027.

Smac-mimetic compound SM-164 induces radiosensitization in breast cancer cells through activation of caspases and induction of apoptosis.
Yang D, et al. Breast Cancer Res Treat 2012 May;133(1):189-99. PMID: 21901386.

Related IAP Products
LCL161

LCL161 is an orally bioavailable SMAC mimetic, potently binds to and inhibits multiple IAPs (i.e. XIAP, c-IAP).

BV6

BV6 is a small-molecule Smac mimetic, which antagonizes IAP proteins.

Birinapant

Birinapant (formerly TL32711) is a Smac mimetic acts as antagonist to cIAP1 and cIAP2.

GDC-0152

GDC-0152 is a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins with potential antineoplastic activity.

AT-406

AT-406 is an orally bioavailable potent IAP (inhibitor of apoptosis protein) of XIAP, cIAP1 and cIAP2 with Ki of 66.4 nM, 1.9 nM and 5.1 nM, respectively.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SM-164 supplier, IAP, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.