2. Anti-infection
  3. Parasite
  4. GSK3186899

GSK3186899  (Synonyms: DDD-853651)

Cat. No.: HY-112622 Purity: 98.61%
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GSK3186899 (DDD-853651) is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay.

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

GSK3186899 Chemical Structure

GSK3186899 Chemical Structure

CAS No. : 1972617-87-0

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1 mg USD 371 In-stock
5 mg USD 780 In-stock
10 mg USD 1250 In-stock
25 mg USD 2550 In-stock
50 mg USD 4050 In-stock
100 mg USD 6450 In-stock
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Based on 1 publication(s) in Google Scholar

GSK3186899 Related Antibodies

Top Publications Citing Use of Products

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

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Description

GSK3186899 (DDD-853651) is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay.

IC50 & Target

CRK12[1].
In Vitro

GSK3186899 (Compound 7) is active against L. donovani in an intra-macrophage assay with an EC50 value of 1.4 μM, and shows good selectivity against mammalian THP-1 host cells (EC50 value>50 μM). This is not as potent as reported data for amphotericin B (EC50 value of 0.07 μM in the intra-macrophage assay), but is comparable to the clinically used drugs miltefosine and paromomycin (EC50 values of 0.9 μM and 6.6 μM, respectively). GSK3186899 is also active in cidal axenic amastigote assay (EC50 value of 0.1 μM). At a concentration of 0.2 μM, GSK3186899 is cytocidal at 96 h; increasing the concentration to 1.8 μM reduced this time to 48 h. GSK3186899 demonstrates a less than 10-fold variation in potency against a panel of Leishmania-derived lines. GSK3186899 is also more active in a panel of Leishmania lines using human peripheral blood mononuclear cells as the host cells[1].

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

GSK3186899 Related Antibodies
In Vivo

In the mouse model of infection, GSK3186899 demonstrates comparable activity to the front-line drug miltefosine, reducing parasite levels by 99% when dosed orally twice a day for 10 days at 25 mg/kg. The efficacy of treatment is dependent on dose, frequency, and duration (10 days better than 5). The non-clinical safety data for GSK3186899 suggests a suitable therapeutic window for progression into regulatory preclinical studies. Non-GLP preclinical assessment of cardiovascular effects and genotoxicity does not reveal any issues that would prevent further development. In addition, there are no notable adverse effects in a rat seven-day repeat-dose oral toxicity study with respect to clinical chemistry and histopathology at all doses tested. Both the in vivo efficacy and safety profile of GSK3186899 support progression to definitive safety studies[1].

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

491.53

Formula

C19H28F3N7O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=S(CCC(F)(F)F)(N[C@H]1CC[C@H](NC2=NC=C3C(NN=C3N4C[C@H](C)OCC4)=N2)CC1)=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 : 250 mg/mL (508.62 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 2.0345 mL 10.1723 mL 20.3446 mL
5 mM 0.4069 mL 2.0345 mL 4.0689 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
×
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 (4.23 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.23 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 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
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 2.0345 mL 10.1723 mL 20.3446 mL 50.8616 mL
5 mM 0.4069 mL 2.0345 mL 4.0689 mL 10.1723 mL
10 mM 0.2034 mL 1.0172 mL 2.0345 mL 5.0862 mL
15 mM 0.1356 mL 0.6782 mL 1.3563 mL 3.3908 mL
20 mM 0.1017 mL 0.5086 mL 1.0172 mL 2.5431 mL
25 mM 0.0814 mL 0.4069 mL 0.8138 mL 2.0345 mL
30 mM 0.0678 mL 0.3391 mL 0.6782 mL 1.6954 mL
40 mM 0.0509 mL 0.2543 mL 0.5086 mL 1.2715 mL
50 mM 0.0407 mL 0.2034 mL 0.4069 mL 1.0172 mL
60 mM 0.0339 mL 0.1695 mL 0.3391 mL 0.8477 mL
80 mM 0.0254 mL 0.1272 mL 0.2543 mL 0.6358 mL
100 mM 0.0203 mL 0.1017 mL 0.2034 mL 0.5086 mL
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GSK3186899 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:

GSK31868991972617-87-0DDD-853651GSK 3186899GSK-3186899DDD853651DDD 853651ParasiteInhibitorinhibitorinhibit

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