1. TGF-beta/Smad
  2. TGF-β Receptor
  3. SM 16

SM 16 

Cat. No.: HY-111482 Purity: 99.96%
Handling Instructions

SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.

For research use only. We do not sell to patients.

SM 16 Chemical Structure

SM 16 Chemical Structure

CAS No. : 614749-78-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 280 In-stock
Estimated Time of Arrival: December 31
50 mg USD 850 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

SM 16 is a ALK5/ALK4 kinase inhibitor with Kis of 10 and 1.5 nM, respectively.

IC50 & Target

Ki: ALK5 (10 nM), ALK4 (1.5 nM)[1]

In Vitro

SM 16 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. SM 16 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). SM 16 exhibits no inhibitory activity against ALK family members ALK1 and ALK6[1].

In Vivo

SM 16 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 SM 16. The growth of established AB12 tumors is significantly inhibited by 5 mg/kg/d SM 16 (P<0.001) delivered via s.c. miniosmotic pumps over 28 days[1].

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 65 mg/mL (150.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3229 mL 11.6144 mL 23.2288 mL
5 mM 0.4646 mL 2.3229 mL 4.6458 mL
10 mM 0.2323 mL 1.1614 mL 2.3229 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.58 mg/mL (5.99 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.58 mg/mL (5.99 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.58 mg/mL (5.99 mM); Clear solution

References
Animal Administration
[1]

Mice[1]

BALB/c mice are injected on the right flank with 1×106 AB12 tumor cells. Mice are randomly divided into two groups and one group is implanted with minipumps loaded with 20% Captisol (control) on the left flank and the other group is implanted with minipumps loaded with 20 mg/mL SM 16. Tumor recurrence is defined as the first day when a tumor is unambiguously visible or palpable. Plasma is obtained under anesthesia and analyzed for SM 16[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

430.50

Formula

C₂₅H₂₆N₄O₃

CAS No.

614749-78-9

SMILES

O=C(C1(CC2)CCC2(C3=NC(C4=CC=C(OCO5)C5=C4)=C(C6=NC(C)=CC=C6)N3)CC1)N

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
SM 16
Cat. No.:
HY-111482
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SM 16

Cat. No.: HY-111482