Zelenirstat (Synonyms: PCLX-001)

Name: Zelenirstat
Brand: MedChemExpress
SKU: HY-147308
Rating: 5.0 (2 reviews)

Cat. No.: HY-147308 Purity: 99.76%: Data Sheet
COA

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

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

CAS No. : 1215011-08-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE Zelenirstat

Cell Proliferation/Viability Assay

: Zelenirstat purchased from MedChemExpress. Usage Cited in: Cancer Res Commun. 2024 Jul 1;4(7):1815-1833. [Abstract]; Detection of PARylation (PAR) by immunoblotting in lysates from (KL/K)MUT cells treated with 1 μmol/L Zelenirstat (NMTi) for 72 hours. Actin, loading control.

: Zelenirstat purchased from MedChemExpress. Usage Cited in: Cancer Res Commun. 2024 Jul 1;4(7):1815-1833. [Abstract]; MIF subcellular localization in (KL/K)MUT H1792 cells treated with vehicle control of 1 μmol/L Zelenirstat (NMTi) for 96 hours and processed for immunofluorescence using a MIF antibody.

: Zelenirstat purchased from MedChemExpress. Usage Cited in: Cancer Res Commun. 2024 Jul 1;4(7):1815-1833. [Abstract]; AIF1 immunoblotting in cytoplasmic and nuclear lysates of (KL/K)MUT H460 treated with 1 μmol/L Zelenirstat (NMTi) o vehicle for 72 hours. Tubulin and lamin staining were used to verify fraction purity.

: Zelenirstat purchased from MedChemExpress. Usage Cited in: Cancer Res Commun. 2024 Jul 1;4(7):1815-1833. [Abstract]; AIF immunofluorescence in tumor sections from (KL/K)MUT H460 xenografts from animals treated with 25 mg/kg Zelenirstat (NMTi) or vehicle control.

: Zelenirstat purchased from MedChemExpress. Usage Cited in: Cancer Res Commun. 2024 Jul 1;4(7):1815-1833. [Abstract]; Cell viability (live/dead reagent) in (KL/K)MUT H460 cells treated with 1 μmol/L Zelenirstat (NMTi) or vehicle control and 20 μmol/L olaparib for 72 hours.

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Biological Activity
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References
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Description

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

Zelenirstat 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].
Zelenirstat (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].
Zelenirstat (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.

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

Zelenirstat (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].
Zelenirstat (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.

1215011-08-7

Appearance

Solid

Color

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 : 8.93 mg/mL (16.61 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
10 mM	0.1860 mL	0.9302 mL	1.8604 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 0.89 mg/mL (1.66 mM); Clear solution

This protocol yields a clear solution of ≥ 0.89 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.9 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: ≥ 0.89 mg/mL (1.66 mM); Clear solution

This protocol yields a clear solution of ≥ 0.89 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.9 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.89 mg/mL (1.66 mM); Clear solution

This protocol yields a clear solution of ≥ 0.89 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.9 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.76%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (249 KB) HNMR (144 KB) RP-HPLC (169 KB) LCMS (387 KB)

Handling Instructions (2659 KB)

References

[1]. Michael Weickert, et al. Initial Characterization and Toxicology of an Nmt Inhibitor in Development for Hematologic Malignancies. Blood. 2019. 134(s1):3362.

[2]. Beauchamp E, et al. Targeting N-myristoylation for therapy of B-cell lymphomas. Nat Commun. 2020 Oct 22;11(1):5348. [Content Brief]

Complete Stock Solution Preparation Table

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

Zelenirstat 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:

Zelenirstat1215011-08-7PCLX-001PCLX001PCLX 001N-myristoyltransferaseNMTorally acitvesmall-moleculeanti-tumorB-cell malignancieslymphomasmyristoyltransferaseB-cell receptorBCRInhibitorinhibitorinhibit

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Zelenirstat (Synonyms: PCLX-001)

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Zelenirstat Related Antibodies

2 Publications Citing Use of MCE Zelenirstat

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Customer Review

Zelenirstat Related Antibodies

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Complete Stock Solution Preparation Table

Zelenirstat Related Classifications

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