2. GPCR/G Protein MAPK/ERK Pathway Apoptosis
  3. Ras Apoptosis
  4. 1A-116

1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo.

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1A-116 Chemical Structure

1A-116 Chemical Structure

CAS No. : 1430208-73-3

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Based on 5 publication(s) in Google Scholar

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Description

1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo[1][2][3].

IC50 & Target

IC50: 4 µM (F3II); 21 µM (MDA-MB-231)[1].
Rac1[1]
Apoptosis[2]
In Vitro

1A-116 (48 h) inhibits F3II and MDA-MB-231 cells proliferation in a concentration-dependent manner with IC50s of 4 μM and 21 μM, respectively[1].
? 1A-116 (1, 10 μM; 12 h) dramatically impaires Rac1 activation, and reduces Rac1-GTP intracellular levels in a concentration-dependent manner in F3II cells[1].
? 1A-116 (50, 100 μM; 12 h) blocks Rac1-P-Rex1 interaction[1].
? 1A-116 (20 μM; 5 h intervals over 25 h) inhibits LN229 cells proliferation in a circadian manner[2].
? 1A-116 (10 μM; 16 h) significantly reduces cell migration at 10 HPS which exhibits temporal dependence. (HPS: After the serum shock, the elapsed time (in hours) is recorded as the hours post-synchronization (HPS))[2].
? 1A-116 (20, 50 μM; 6 h) induces cells apoptosis and in a circadian-dependent manner[2].
? 1A-116 (100 nM) decreases the thickness of the epidermal layers of Vav2 and Rac1-mediated hyperplasia, but not the PAK1-mediated one, which exhibits the activity of inhibiting Rac1 at the GEF-Rac1 level[3].

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

1A-116 Related Antibodies

Cell Proliferation Assay[1][2]

Cell Line: MDA-MB-231, F3II, LN229 cells
Concentration: 20 µM
Incubation Time: 48 h; 5 h intervals over 25 h.
Result: Inhibited cell proliferation in a concentration-dependent and circadian manner.

Cell Viability Assay[3]

Cell Line: Ker-CT human keratinocytes cells with oncogenic Vav2/Rac1 F28L/PAK1 Tyrosine 423
Concentration: 100 nM
Incubation Time:
Result: Inhibited Rac1 activity at the GEF-Rac1 level.

Cell Migration Assay [2]

Cell Line: LN229 cells
Concentration: 10 µM
Incubation Time: 16 h
Result: Reduced cell migration at 10 HPS which exhibited temporal dependence.

Apoptosis Analysis[2]

Cell Line: LN229 cells
Concentration: 20, 50 µM
Incubation Time: 6 h
Result: Induced cells apoptosis and in a circadian-dependent manner.

Western Blot Analysis[1]

Cell Line: F3II cells
Concentration: 1, 10 µM
Incubation Time: 12 h
Result: Blocked Rac1-P-Rex1 interaction.
Reduced Rac1-GTP intracellular levels in a concentration-dependent manner.
In Vivo

1A-116 (3 mg/kg; i.v.; once a day for 21 days) demonstrates a high antimetastatic activity with about 60% formation reduction of total metastatic lung colonies in vivo and shows no apparent toxicity[1].
? 1A-116 (20 mg/kg; i.p.; once a day, 73 days for ZT12, 68 days for ZT3) increases survival time when treated at ZT12 compare to ZT3 in tumor-bearing mice. (ZT: Zeitgeber time 12 (ZT12) defined as the time of lights off (local time 7 p.m.) and ZT0 defined as lights on (local time 7 a.m.))[2].
? 1A-116 shows good oral availability[3].

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

Animal Model: Female BALB/c inbred mice (8 to 10-week-old; average 20 g)[1]
Dosage: 3 mg/kg
Administration: Intravenous injection; once a day for 21 days.
Result: Demonstrated a high antimetastatic activity.
Animal Model: Male NIH Swiss foxN1(∆/∆) nude mice (2-month-old; GBM model)[2].
Dosage: 20 mg/kg
Administration: Intraperitoneal injection (at ZT3, ZT12); once a day, 73 days for ZT12, 68 days for ZT3.
Result: Increased survival time when treated at ZT12 compared to ZT3 in tumor-bearing mice.
Molecular Weight

307.31

Formula

C16H16F3N3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=C(NC1=CC=CC=C1C(F)(F)F)NC2=CC(C)=CC(C)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (325.40 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 3.2540 mL 16.2702 mL 32.5404 mL
5 mM 0.6508 mL 3.2540 mL 6.5081 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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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: ≥ 2.5 mg/mL (8.14 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (8.14 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2540 mL 16.2702 mL 32.5404 mL 81.3511 mL
5 mM 0.6508 mL 3.2540 mL 6.5081 mL 16.2702 mL
10 mM 0.3254 mL 1.6270 mL 3.2540 mL 8.1351 mL
15 mM 0.2169 mL 1.0847 mL 2.1694 mL 5.4234 mL
20 mM 0.1627 mL 0.8135 mL 1.6270 mL 4.0676 mL
25 mM 0.1302 mL 0.6508 mL 1.3016 mL 3.2540 mL
30 mM 0.1085 mL 0.5423 mL 1.0847 mL 2.7117 mL
40 mM 0.0814 mL 0.4068 mL 0.8135 mL 2.0338 mL
50 mM 0.0651 mL 0.3254 mL 0.6508 mL 1.6270 mL
60 mM 0.0542 mL 0.2712 mL 0.5423 mL 1.3559 mL
80 mM 0.0407 mL 0.2034 mL 0.4068 mL 1.0169 mL
100 mM 0.0325 mL 0.1627 mL 0.3254 mL 0.8135 mL
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1A-116 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

1A-1161430208-73-3RasApoptosisRho GTPasesRac1-P-Rex1TIAM1EGFcircadian rhythmsInhibitorinhibitorinhibit

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