2. Cell Cycle/DNA Damage Anti-infection
  3. DNA/RNA Synthesis Parasite
  4. DDD85646

DDD85646 (IMP-366) is an orally active of trypanosoma brucei N-myristoyltransferase (TbNMT IC50=2 nM; hNMT IC50=4 nM). The enzyme N-myristoyltransferase (NMT) is a potential agent target for human African trypanosomiasis.

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DDD85646 Chemical Structure

DDD85646 Chemical Structure

CAS No. : 1215010-55-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 418 In-stock
Solution
10 mM * 1 mL in DMSO USD 418 In-stock
Solid
1 mg USD 120 In-stock
5 mg USD 380 In-stock
10 mg USD 590 In-stock
25 mg USD 1180 In-stock
50 mg USD 1850 In-stock
100 mg USD 2960 In-stock
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Based on 1 publication(s) in Google Scholar

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

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Description

DDD85646 (IMP-366) is an orally active of trypanosoma brucei N-myristoyltransferase (TbNMT IC50=2 nM; hNMT IC50=4 nM). The enzyme N-myristoyltransferase (NMT) is a potential agent target for human African trypanosomiasis[1][2][3][4].

IC50 & Target

Trypanosoma

 

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
2.8 μM
Compound: 1; MMV688180
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
[PMID: 30647879]
MRC5 EC50
0.002 μM
Compound: 1
Antitrypanosomal activity against Trypanosoma brucei BSF427 expressing VSG118 infected in human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
Antitrypanosomal activity against Trypanosoma brucei BSF427 expressing VSG118 infected in human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
[PMID: 25412409]
MRC5 EC50
0.3 μM
Compound: 1
Antiproliferative activity against human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
Antiproliferative activity against human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
[PMID: 25412409]
MRC5 EC50
0.4 μM
Compound: 1; DDD85646
CYtotoxicity against human MRC5 cells after 69 hrs by resazurin assay
CYtotoxicity against human MRC5 cells after 69 hrs by resazurin assay
[PMID: 29125744]
In Vitro

DDD85646 (50 nM) female NMRI mouse model showed significant antitrypanosomic activity[3].
DDD85646 (0-100 nM; 6, 24h) has a targeting effect in Trypanosoma brucei, and can effectively inhibit the N-myristyl transferase (TbNMT) of bloodstream type Trypanosoma Brucei, and this inhibition is directly related to the inhibition of proliferation of Trypanosoma Brucei[3].
DDD85646 has an IC50 value of 4.4 nM for L. donovani NMT and an EC50 value of 8µM for L. donovani extracellular amastigotes[3].

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

DDD85646 Related Antibodies
In Vivo

DDD85646 (10, 50 mg/kg; Oral administration; 1) has moderate bioavailability (about 20%) in female NMRI mouse models, and the free drug level is higher than EC99 (EC99 is about 6 nM), which can effectively inhibit the proliferation of T. b. brucei[3].
DDD85646 (0-50 mg/kg; Oral administration; Twice a day; 4 days) kills Trypanosoma brucei by acting on TbNMT in T. b. brucei acute mouse model of HAT[3].
DDD85646 (50 mg/kg; Oral administration; Twice a day) shows significant antitrypanosomic activity in female NMRI mice models[3].

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

Animal Model: T. b. brucei acute mouse model of HAT[3]
Dosage: 0-50 mg/kg
Administration: Oral gavage (p.o.)
Result: Cured all animals in the T. b. brucei acute mouse model of HAT at a minimal oral dose of 12.5 mg/kg (b.i.d. for 4 days)
Prevented 99% of T. b. brucei proliferation
Parasite numbers dropped below detectable levels within 12 hours
Molecular Weight

495.43

Formula

C21H24Cl2N6O2S
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=S(C1=C(Cl)C=C(C2=CC(N3CCNCC3)=NC=C2)C=C1Cl)(NC4=C(C)N(C)N=C4C)=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 : 100 mg/mL (201.84 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 2.0184 mL 10.0922 mL 20.1845 mL
5 mM 0.4037 mL 2.0184 mL 4.0369 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: ≥ 2.5 mg/mL (5.05 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 (5.05 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 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 2.0184 mL 10.0922 mL 20.1845 mL 50.4612 mL
5 mM 0.4037 mL 2.0184 mL 4.0369 mL 10.0922 mL
10 mM 0.2018 mL 1.0092 mL 2.0184 mL 5.0461 mL
15 mM 0.1346 mL 0.6728 mL 1.3456 mL 3.3641 mL
20 mM 0.1009 mL 0.5046 mL 1.0092 mL 2.5231 mL
25 mM 0.0807 mL 0.4037 mL 0.8074 mL 2.0184 mL
30 mM 0.0673 mL 0.3364 mL 0.6728 mL 1.6820 mL
40 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2615 mL
50 mM 0.0404 mL 0.2018 mL 0.4037 mL 1.0092 mL
60 mM 0.0336 mL 0.1682 mL 0.3364 mL 0.8410 mL
80 mM 0.0252 mL 0.1262 mL 0.2523 mL 0.6308 mL
100 mM 0.0202 mL 0.1009 mL 0.2018 mL 0.5046 mL
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DDD85646 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:

DDD856461215010-55-1IMP-366DDD 85646DDD-85646IMP366IMP 366DNA/RNA SynthesisParasitetrypanosoma bruceiN-myristoyltransferaseNMTAfrican trypanosomiasisInhibitorinhibitorinhibit

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