SM16

SM16 is a novel Type I TGF-β signaling inhibitor.

Product information

CAS Number: 614749-78-9

Molecular Weight: 430.50

Formula: C25H26N4O3

Chemical Name: 4-[4-(1,3-Benzodioxol-5-yl)-5-(6-methyl-2-pyridinyl)-1H-imidazol-2-yl]-bicyclo[2.2.2]octane-1-carboxamide

Smiles: CC1=CC=CC(=N1)C1NC(=NC=1C1=CC2OCOC=2C=C1)C12CCC(CC1)(CC2)C(N)=O

InChiKey: JUHTXZGCTPDXRU-UHFFFAOYSA-N

InChi: InChI=1S/C25H26N4O3/c1-15-3-2-4-17(27-15)21-20(16-5-6-18-19(13-16)32-14-31-18)28-23(29-21)25-10-7-24(8-11-25,9-12-25)22(26)30/h2-6,13H,7-12,14H2,1H3,(H2,26,30)(H,28,29)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

SM16 inhibits TGFβ-induced plasminogen activator inhibitor-luciferase activity (IC50=64 nM) and TGFβ- or activin-induced Smad2 phosphorylation at concentrations between 100 and 620 nM. SM16 is tested against >60 related and unrelated kinases and shows moderate off-target activity only against Raf (IC50=1 μM) and p38/SAPKa (IC50=0.8 μM). SM16 exhibits no inhibitory activity against ALK family members ALK1 and ALK6.

In Vivo:

SM16 penetrates tumor cells in vivo, suppressing tumor phosphorylated Smad2/3 levels for at least 3 h following treatment of tumor-bearing mice with a single i.p. bolus of 20 mg/kg SM16. The growth of established AB12 tumors is significantly inhibited by 5 mg/kg/d SM16 (P<0.001) delivered via s.c. miniosmotic pumps over 28 days.

References:

1. Wongwaree S, Daengsuwan T. Comparison efficacy of randomized nebulized magnesium sulfate and ipratropium bromide/fenoterol in children with moderate to severe asthma exacerbation. Asian Pac J Allergy Immunol. 2019 Aug 18. doi: 10.12932/AP-190717-0118. Epub ahead of print. PMID: 31421659.
2. Pozzoli C, Bertini S, Poli E, Placenza G, Menozzi A. Relaxing effects of clenbuterol, ritodrine, salbutamol and fenoterol on the contractions of horse isolated bronchi induced by different stimuli. Res Vet Sci. 2020 Feb;128:43-48. doi: 10.1016/j.rvsc.2019.10.022. Epub 2019 Oct 31. PMID: 31710963.
3. Stoiber B, Haslinger C, Schäffer MK, Zimmermann R, Schäffer L. Effect of dual tocolysis with fenoterol and atosiban in human myometrium. J Perinat Med. 2019 Feb 25;47(2):190-194. doi: 10.1515/jpm-2018-0010. PMID: 30218606.

Products are for research use only. Not for human use.