SM-164 Hydrochloride

SM-164 Hydrochloride
Cat. No. : CS-0041048
M. Wt. : 1157.88
Size Stock Price Quantity Add to Cart Quotation Online
5mg In-stock $350.0
10mg In-stock $600.0
50mg In-stock $1800.0
Products are for research use only. Not for human use. We do not sell to patients.

Bulk Inquiry

Your information is safe with us. * Required Fields
  • Dr.
  • Prof.
  • Mr.
  • Ms.
  • Mrs.
  • Miss.
*Country or Region:
  • United States
  • Canada
  • United Kingdom
  • Australia
  • China
  • Germany
  • France
  • Japan
  • Korea South
  • Switzerland
  • ----------------------------------
  • Albania
  • Algeria
  • Argentina
  • Armenia
  • Australia
  • Austria
  • Azerbaijan
  • Bahrain
  • Bangladesh
  • Barbados
  • Belarus
  • Belgium
  • Bolivia
  • Bosnia Herzegovina
  • Brazil
  • Bulgaria
  • Cameroon
  • Canada
  • Chile
  • China
  • Colombia
  • Croatia
  • Cyprus
  • Czech Republic
  • Denmark
  • Ecuador
  • Egypt
  • Estonia
  • Fiji
  • Finland
  • France
  • Georgia
  • Germany
  • Gibraltar
  • Greece
  • Hungary
  • Iceland
  • India
  • Indonesia
  • Iran
  • Iraq
  • Ireland
  • Israel
  • Italy
  • Japan
  • Jordan
  • Kazakhstan
  • Kenya
  • Korea South
  • Kuwait
  • Latvia
  • Lebanon
  • Libya
  • Lithuania
  • Luxembourg
  • Macedonia
  • Malaysia
  • Malta
  • Mexico
  • Moldova
  • Monaco
  • Mongolia
  • Montenegro
  • Morocco
  • Nepal
  • Netherlands
  • New Zealand
  • Nigeria
  • Norway
  • Oman
  • Pakistan
  • Paraguay
  • Peru
  • Philippines
  • Poland
  • Portugal
  • Puerto Rico
  • Qatar
  • Republic of Benin
  • Romania
  • Russia
  • Saudi Arabia
  • Serbia
  • Singapore
  • Slovakia
  • Slovenia
  • South Africa
  • Spain
  • Sri Lanka
  • Suriname
  • Sweden
  • Switzerland
  • Syria
  • Thailand
  • Tunisia
  • Turkey
  • Ukraine
  • United Arab Emirates
  • United Kingdom
  • United States
  • Uruguay
  • Uzbekistan
  • Venezuela
  • Vietnam
  • Zambia
  • Zimbabwe
  • Other Countries
* Applicant name:
* Organization Name:
* Email address:
* Requested quantity:
  • mg
  • ug
  • g
  • kg
  • t
  • mL
  • L
* Phone number:
Organization Name, 
Email address, 
Requested quantity, 
Phone number, 
  • Data Sheet

  • Introduction

  • SDS

  • COA & Spectra

Name: SM-164 Hydrochloride; 
Cat. No. : CS-0041048
CAS No. :    
Formula: C62H85ClN14O6
M. Wt. : 1157.88
Solubility: H2O: ≥ 106 mg/mL


SM-164 Hydrochloride is a cell-permeable Smac mimetic compound. SM-164 binds to XIAP protein containing both the BIR2 and BIR3 domains with an IC50 value of 1.39 nM and functions as an extremely potent antagonist of XIAP. IC50 & Target: IC50: 1.39 nM (XIAP)[1]
Ki: 0.56 nM to (XIAP), 0.31 nM to (cIAP-1), 1.1 nM (cIAP-2)[2] In Vitro: SM-164 is a non-peptide, cell-permeable, bivalent small-molecule, which mimics Smac protein for targeting XIAP. SM-164 binds to XIAP containing both BIR domains with an IC50 value of 1.39 nM, being 300 and 7000-times more potent than its monovalent counterparts and the natural Smac AVPI peptide, respectively. SM-164 concurrently interacts with both BIR domains in XIAP and functions as an ultra-potent antagonist of XIAP in both cell-free functional and cell-based assays. SM-164 targets cellular XIAP and effectively induces apoptosis at concentrations as low as 1 nM in leukemia cancer cells, while having a minimal toxicity to normal human primary cells at 10,000 nM[1]. The binding affinities of SM-164 to XIAP, cIAP-1, and cIAP-2 proteins are determined using fluorescence-polarization based assays. SM-164 has a Ki value of 0.56 nM to XIAP protein containing both BIR2 and BIR3 domains. SM-164 has a Ki value of 0.31 nM to cIAP-1 protein containing both BIR2 and BIR3 domains. SM-164 binds to cIAP-2 BIR3 protein with Ki values of 1.1 nM. Addition of exogenous TNFα can significantly enhance the activity of these Smac mimetics, especially for SM-164, in resistant cancer cell lines such as HCT116 and MDA-MB-453[2]. In Vivo: SM-164 is evaluated for its ability to inhibit tumor growth. SM-164 is highly effective in inhibition of tumor growth and capable of achieving tumor regression in the MDA-MB-231 xenograft model. Treatment with SM-164 at 1 mg/kg completely inhibits tumor growth during the treatment. Treatment with SM-164 at 5 mg/kg reduces the tumor volume from 147±54 mm3 at the beginning of the treatment (day 25) to 54±32 mm3 at the end of the treatment (day 36), a reduction of 65%. The strong antitumor activity by SM-164 is long lasting and not transient. SM-164 at 5 mg/kg is statistically more effective than Taxotere at the end of the treatment (P<0.01) or when the tumor size in the control group reaches 750 mm3 (P<0.02)[2].


Kinase Assay: [2]A set of sensitive and quantitative fluorescence polarization (FP)-based assays are developed to determine the binding affinities of our designed Smac mimetics to XIAP BIR3, XIAP containing both BIR2 and BIR3 domains, cIAP-1 BIR3, cIAP-1 containing both BIR2 and BIR3 domains, and cIAP-2 protein. The FP-based assay for XIAP BIR3 protein is measured. Briefly, 5-carboxyfluorescein is coupled to the lysine side chain of a mutated Smac peptide with the sequence (AbuRPFK-Fam) and this fluorescently tagged peptide (named SM5F) is used as the fluorescent tracer in FP-based binding assay to XIAP BIR3. The Kd value of this fluorescent tracer is determined to be 17.9 nM to XIAP BIR3. In competitive binding experiments, a tested compound is incubated with 30 nM of XIAP BIR3 protein and 5 nM of SM5F in the assay buffer (100 mM potassium phosphate, pH 7.5; 100μg/mL bovine gamma globulin; 0.02 % sodium azide)[2].
Cell Assay: [2]HCT116 colon cancer cells are treated with SM-164 (1, 10, and 100 nM) alone, TNFα alone, or the combination for 48 h. Cell growth inhibition is determined by a WST assay[2].
Animal Administration: [2]Mice[2]
SCID mice (8-10 per group) bearing MDA-MB-231 xenograft tumors are treated i.v. with 1 and 5 mg/kg of SM-164 or 7.5 mg/kg of Taxotere or vehicle control daily, 5 d/wk for 2 wk. Tumor sizes and animal weights are measured thrice a week[2].


Sun H, et al. Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP. J Am Chem Soc. 2007 Dec 12;129(49):15279-94.

Lu J, et al. SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP. Cancer Res. 2008 Nov 15;68(22):9384-93.

Enter Lot Number:

We apologize for the inconvenience. The Certificate of Analysis you requested is not currently available on-line:

1. The Lot Number you requested may have been entered incorrectly. How to get a Lot Number

2. The COA of the Lot you requested has not been added to our database.

Browsing History
    Tags:SM-164 Hydrochloride supplier,SM-164 Hydrochloride purchase,SM-164 Hydrochloride manufacturer,SM-164 Hydrochloride sigma,SM-164 Hydrochloride distributor,cost,SM-164 Hydrochloride buy,SM-164 Hydrochloride for sale
    Please enter your email address
    Organization name: Email:

    Submit success

    No information on this batch number
    How to get a Lot Number

    Lot numbers can be found on the outside label of a product:

    ChemScene Label