2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. Z62954982

Z62954982  (Synonyms: ZINC08010136)

Cat. No.: HY-115376 Purity: 98.89%
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Z62954982 (ZINC08010136) is a potent, selective and cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982 disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA).

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

Z62954982 Chemical Structure

Z62954982 Chemical Structure

CAS No. : 1090893-12-1

Size Price Stock Quantity
5 mg USD 110 In-stock
10 mg USD 170 In-stock
25 mg USD 340 In-stock
50 mg USD 550 In-stock
100 mg USD 880 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Z62954982 (ZINC08010136) is a potent, selective and cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982 disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA)[1][2].

In Vitro

Z62954982 (5-100 μM; 4 hours) reduces the intracellular levels of Rac1- GTP in a concentration-dependent manner,and shows the most potent inhibitory action with an IC50 of 12.2 μM in Human SMCs[1].
Z62954982 (25 μM; 4 hours) significantly reduces the ratio Rac1-GTP/Rac1 and has the most potent inhibitory action (86.0%) in cultured SMCs[1].
Z62954982 (10-100 μM; 72 hours) causes a concentration-dependent decrease in transendothelial electrical resistance (TER) in both HDMEC and HUVEC monolayers[2].

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

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In Vivo

Z62954982 (intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks) has no obvious signs of toxicity and decreases both phosphorylation of p38 as well as secreted IL-6 in PASMCs in response to hypoxia in both abr-/- and bcr-/- mice[3].

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

Animal Model: Male bcr-/-, abr-/- and wt mice (8 to 10-week-old littermates) are exposed to hypoxia (10% O2) or normoxia (21% O2) for 3 weeks[3]
Dosage: 10 mg/kg or 20 mg/kg
Administration: Intraperitoneal injection; 10 mg/kg every other day or 20 mg/kg daily; 3 weeks
Result: Promoted phosphorylation of p38 MAPK and increased IL-6 in Hypoxia in mice.
Molecular Weight

415.46

Formula

C20H21N3O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C)C(S(=O)(N)=O)=C1)C2=CC=CC(OCC3=C(C)ON=C3C)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 14.29 mg/mL (34.40 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 2.4070 mL 12.0349 mL 24.0697 mL
5 mM 0.4814 mL 2.4070 mL 4.8139 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.

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

Mass
=
Concentration
×
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: 1.43 mg/mL (3.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 1.43 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: 1.43 mg/mL (3.44 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 1.43 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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:

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, . 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

Purity: ≥99.0%

COA (247 KB)

Handling Instructions (2659 KB)
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 2.4070 mL 12.0349 mL 24.0697 mL 60.1743 mL
5 mM 0.4814 mL 2.4070 mL 4.8139 mL 12.0349 mL
10 mM 0.2407 mL 1.2035 mL 2.4070 mL 6.0174 mL
15 mM 0.1605 mL 0.8023 mL 1.6046 mL 4.0116 mL
20 mM 0.1203 mL 0.6017 mL 1.2035 mL 3.0087 mL
25 mM 0.0963 mL 0.4814 mL 0.9628 mL 2.4070 mL
30 mM 0.0802 mL 0.4012 mL 0.8023 mL 2.0058 mL
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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:

Z629549821090893-12-1ZINC08010136Z 62954982Z-62954982ZINC 08010136ZINC-08010136RasPDGF-BBaorticSMCbaselineendothelialbarrierintegrityRac1/Tiam1Inhibitorinhibitorinhibit

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