2. Metabolic Enzyme/Protease
  3. N-myristoyltransferase
  4. PCLX-001

PCLX-001 is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively. PCLX-001 can induce cell apoptosis, has anti-cancer activity, inhibits early B cell receptor (BCR) signaling, and can be used to study malignant lymphoma.

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PCLX-001 Chemical Structure

PCLX-001 Chemical Structure

CAS No. : 1215011-08-7

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1 mg USD 280 In-stock
5 mg USD 700 In-stock
10 mg USD 960 In-stock
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Based on 2 publication(s) in Google Scholar

PCLX-001 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PCLX-001 is an orally acitve, small-molecule, dual N-myristoyltransferase (NMT) inhibitor, with IC50s of 5 nM (NMT1) and 8 nM (NMT2), respectively. PCLX-001 can induce cell apoptosis, has anti-cancer activity, inhibits early B cell receptor (BCR) signaling, and can be used to study malignant lymphoma[1][2].

Cellular Effect
Cell Line Type Value Description References
MRC5 EC50
0.0004 μM
Compound: 6
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
0.09 μM
Compound: 6
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]
In Vitro

PCLX-001 does not inhibit any kinase at 10 µM (5380 ng/mL) and shows moderate inhibition of three kinases (MRCKA, PIP5K2B and SRPK1) at 100 µM (53800 ng/mL)[1].
PCLX-001 (0-10 μM, 4 days) inhibits the proliferation of tumor cells such as BL2 and DOHH2, but has no effect on normal cells IM9[2].
PCLX-001 (0-1 μM, 1 h) reduces total protein myristoylation in IM9 and BL2 and induces apoptosis of lymphoma cells[2].

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

PCLX-001 Related Antibodies

Cell Viability Assay[2]

Cell Line: IM9, VDS, BL2, Ramos, BJAB, DOHH2, WSU-DLCL2, SU-DHL-10
Concentration: 0.001, 0.01, 0.1, 1, 10 μM; 0, 0.005, 0.01, 0.05, 0.1, 0.5, 1, 5 μM
Incubation Time: 96 h; 4 days
Result: Inhibited tumor cell proliferation in a time- and dose-dependent manner and had no effect on normal cells.

Western Blot Analysis[2]

Cell Line: BL2, IM9
Concentration: 0, 0.01, 0.05, 0.1, 0.5, 1 μM
Incubation Time: 1 h; 72 h
Result: Reduced total protein myristoylation was more sensitive in malignant tumors. Both Src and Lyn SFK protein levels showed more obvious dose- and time-dependent decreases.
In Vivo

PCLX-001 (5-1000 mg/kg, oral, once daily, 14-21 days) has an MTD of 50 mg/kg in a 21-day study in mice, >75 mg/kg in a 14-day study in rats, and between 5 and 25 mg/kg in a 14-day study in dogs[1].
PCLX-001 (0-50 mg/kg, subcutaneous injection, once daily; 0-15 days) induces tumor regression in BL2 xenograft mice[2].

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

Animal Model: Mice, rats, dogs[1]
Dosage: 5-1000 mg/kg; daily; 14 and 21 days
Administration: Oral
Result: Showed that a single dose of 50 mg/kg caused vomiting, diarrhea, and weight loss in dogs, while a single dose of 1000 mg/kg caused the death of one rat and complete regression of xenograft tumors in mice.
Animal Model: BL2 xenograft mice[2]
Dosage: 0, 10, 20, 50 mg/kg; daily; 0, 5, 10, 15 days
Administration: Subcutaneous injection (s.c.)
Result: Reduced tumor volume and caused complete tumor regression, and prolonged the survival of BL2 tumor-bearing mice.
Clinical Trial
Molecular Weight

537.51

Formula

C24H30Cl2N6O2S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=S(NC1=C(C)N(C)N=C1CC(C)C)(C2=C(Cl)C=C(C3=CC(N4CCNCC4)=NC=C3)C=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 : 10 mg/mL (18.60 mM; ultrasonic and warming and heat to 60°C; 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 1.8604 mL 9.3022 mL 18.6043 mL
5 mM 0.3721 mL 1.8604 mL 3.7209 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
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Concentration
×
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

×
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 mg/mL (1.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (1.86 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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 1.8604 mL 9.3022 mL 18.6043 mL 46.5108 mL
5 mM 0.3721 mL 1.8604 mL 3.7209 mL 9.3022 mL
10 mM 0.1860 mL 0.9302 mL 1.8604 mL 4.6511 mL
15 mM 0.1240 mL 0.6201 mL 1.2403 mL 3.1007 mL
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PCLX-001 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:

PCLX-0011215011-08-7PCLX001PCLX 001N-myristoyltransferaseNMTorally acitvesmall-moleculeanti-tumorB-cell malignancieslymphomasmyristoyltransferaseB-cell receptorBCRInhibitorinhibitorinhibit

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