1. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  2. MAP3K Src FGFR Ribosomal S6 Kinase (RSK) LIM Kinase (LIMK)
  3. SM1-71

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.

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

SM1-71 Chemical Structure

SM1-71 Chemical Structure

CAS No. : 2088179-99-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 78 In-stock
Solution
10 mM * 1 mL in DMSO USD 82 In-stock
Solid
5 mg USD 80 In-stock
10 mg USD 130 In-stock
25 mg USD 250 In-stock
50 mg USD 400 In-stock
100 mg USD 650 In-stock
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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines[1][2][3].

IC50 & Target

LIMK1

 

RSK2

 

Cellular Effect
Cell Line Type Value Description References
ASPC1 IC50
18 nM
Compound: 5
Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human AsPC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
[PMID: 28038940]
BaF3 IC50
3 nM
Compound: 5
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs in presence of IL-3 by CellTiter-Glo assay
[PMID: 28038940]
BaF3 IC50
5 nM
Compound: 5
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against mouse BA/F3 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
[PMID: 28038940]
BaF3 IC50
7 nM
Compound: 5
Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against mouse BA/F3 cells after 72 hrs by CellTiter-Glo assay
[PMID: 28038940]
PANC-1 IC50
410 nM
Compound: 5
Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human PANC1 cells harboring KRAS G12D mutant after 72 hrs by CellTiter-Glo assay
[PMID: 28038940]
SK-CO-1 IC50
29 nM
Compound: 5
Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human SKCO1 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
[PMID: 28038940]
SW-620 IC50
67 nM
Compound: 5
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant after 72 hrs by CellTiter-Glo assay
[PMID: 28038940]
In Vitro

SM1-71 (0.001-100 μM; 72 h) potently inhibits the proliferation of H23 and Calu-6 non-small cell lung cancer cell lines with a concentration-dependent manner[1].
SM1-71 (72 h) induces potent cytotoxicity with nanomolar values for GR50 and negative GRmax values in eight of 11 cancer cell lines[2].

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

Cell Viability Assay[1]

Cell Line: H23-KRASG12C and Calu-6-KRASQ61K cells
Concentration: 0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 72 hours
Result: Inhibited proliferation of H23-KRASG12C and Calu-6-KRASQ61K cells with IC50s of 0.4 and 0.3 μM, respectively.
Molecular Weight

463.96

Formula

C24H26ClN7O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C=CC(NC1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=O

Shipping

Room temperature in continental US; may vary elsewhere.

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 : 125 mg/mL (269.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1554 mL 10.7768 mL 21.5536 mL
5 mM 0.4311 mL 2.1554 mL 4.3107 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (4.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.48 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 96.09%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1554 mL 10.7768 mL 21.5536 mL 53.8840 mL
5 mM 0.4311 mL 2.1554 mL 4.3107 mL 10.7768 mL
10 mM 0.2155 mL 1.0777 mL 2.1554 mL 5.3884 mL
15 mM 0.1437 mL 0.7185 mL 1.4369 mL 3.5923 mL
20 mM 0.1078 mL 0.5388 mL 1.0777 mL 2.6942 mL
25 mM 0.0862 mL 0.4311 mL 0.8621 mL 2.1554 mL
30 mM 0.0718 mL 0.3592 mL 0.7185 mL 1.7961 mL
40 mM 0.0539 mL 0.2694 mL 0.5388 mL 1.3471 mL
50 mM 0.0431 mL 0.2155 mL 0.4311 mL 1.0777 mL
60 mM 0.0359 mL 0.1796 mL 0.3592 mL 0.8981 mL
80 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6735 mL
100 mM 0.0216 mL 0.1078 mL 0.2155 mL 0.5388 mL
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Product Name:
SM1-71
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