HZX-02-059 (Synonyms: Methuosis inducer 1)

Name: HZX-02-059
Brand: MedChemExpress
SKU: HY-112440
Rating: 4.5 (0 reviews)

Cat. No.: HY-112440 Purity: 99.40%: Data Sheet
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HZX-02-059 is an allosteric inhibitor of PIKFYVE, and a methuosis inducer. HZX-02-059 disrupts the PIKfyve/TFEB axis, suppresses tubulin polymerization, reduces phosphorylated mTOR levels, downregulates p53, PI3K/AKT, c-Myc, and NF-κB pathways. HZX-02-059 induces G₂/M cell cycle arrest, apoptosis, and inhibits cancer cell proliferation. HZX-02-059 can be used for the research of lymphoma, double-hit lymphoma, and B-cell acute lymphoblastic leukemia.

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

HZX-02-059 Chemical Structure

CAS No. : 2240205-30-3

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Methuosis^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.326 μM Compound: 13	Antiproliferative activity against human A375 cells after 48 hrs by MTS assay Antiproliferative activity against human A375 cells after 48 hrs by MTS assay	[PMID: 29878764]
A549	IC₅₀	1.892 μM Compound: 13	Antiproliferative activity against human A549 cells after 48 hrs by MTS assay Antiproliferative activity against human A549 cells after 48 hrs by MTS assay	[PMID: 29878764]
BGC-823	IC₅₀	1.566 μM Compound: 13	Antiproliferative activity against human BGC823 cells after 48 hrs by MTS assay Antiproliferative activity against human BGC823 cells after 48 hrs by MTS assay	[PMID: 29878764]
HCT-116	IC₅₀	1.008 μM Compound: 13	Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTS assay	[PMID: 29878764]
HeLa	IC₅₀	1 μM Compound: D-13	Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay	[PMID: 38117948]
HepG2	IC₅₀	1.197 μM Compound: 13	Antiproliferative activity against human HepG2 cells after 48 hrs by MTS assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTS assay	[PMID: 29878764]
MCF-10A	IC₅₀	>10 μM Compound: 13	Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 48 hrs by MTS assay Cytotoxicity against human MCF10A cells assessed as reduction in cell viability after 48 hrs by MTS assay	[PMID: 29878764]
MCF7	IC₅₀	2.611 μM Compound: 13	Antiproliferative activity against human MCF7 cells after 48 hrs by MTS assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTS assay	[PMID: 29878764]
MDA-MB-231	IC₅₀	0.78 μM Compound: D-13	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability incubated for 24 hrs by CCK8 assay	[PMID: 38117948]
MDA-MB-231	IC₅₀	1.571 μM Compound: 13	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTS assay Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by MTS assay	[PMID: 29878764]
MDA-MB-435S	IC₅₀	2.268 μM Compound: 13	Antiproliferative activity against human MDA-MB-435S cells after 48 hrs by MTS assay Antiproliferative activity against human MDA-MB-435S cells after 48 hrs by MTS assay	[PMID: 29878764]
SK-MEL-28	IC₅₀	1.37 μM Compound: 13	Antiproliferative activity against human SK-MEL-28 cells after 48 hrs by MTS assay Antiproliferative activity against human SK-MEL-28 cells after 48 hrs by MTS assay	[PMID: 29878764]
SK-MEL-30	IC₅₀	1.662 μM Compound: 13	Antiproliferative activity against human SK-MEL-30 cells after 48 hrs by MTS assay Antiproliferative activity against human SK-MEL-30 cells after 48 hrs by MTS assay	[PMID: 29878764]

In Vitro

HZX-02-059 (1 µM) binds potently to PIKFYVE (K_d = 10 nM) and strongly inhibits PIKFYVE and seven additional kinases by 99%, while inhibiting PIP4K2C by 60%^[1].
HZX-02-059 reduces the viability of lymphoma cell lines in vitro with a median IC₅₀ of 0.19 µM^[1].
HZX-02-059 (1 μM) binds potently to purified PIKfyve kinase with a K_d of 10 nM^[2].
HZX-02-059 (100 μM) inhibits purified tubulin polymerization^[2].
HZX-02-059 (2 μM; 8 h) inhibits PIKfyve activity in 293T cells, reducing PI(3,5)P₂ levels and altering late endosome/lysosome localization^[2].
HZX-02-059 (48-72 h) potently inhibits proliferation of Will-2, LR, and TMD8 DHL cell lines in a dose- and time-dependent manner, with IC₅₀ values ranging from 107 nM (Will-2, 72 h) to 344 nM (TMD8, 48 h)^[2].
HZX-02-059 (0.25-4 μM; 24-72 h) induces caspase-independent cell death in Will-2, LR, and TMD8 DHL cell lines in a dose- and time-dependent manner, primarily via late apoptotic-like cell death^[2].
HZX-02-059 (10 nM-2 μM; 6 h-5 days) triggers methuosis in Will-2 DHL cells via inhibition of the PIKfyve/TFEB axis, inducing characteristic vacuolation, reducing TFEB expression, and disrupting autophagy^[2].
HZX-02-059 (0.25-1 μM; 24 h) induces G₂/M phase cell cycle arrest in Will-2, LR, and TMD8 DHL cell lines, via inhibition of tubulin and suppression of the mTOR/Myc axis^[2].
HZX-02-059 (0-4 μM; 72 h) does not induce apoptosis in primary PBMCs from healthy donors, indicating low toxicity toward normal hematopoietic cells^[2].
HZX-02-059 (48-72 h) potently inhibits proliferation of Nalm6 and Sup-B15 B-ALL cells with IC₅₀ values ranging from 376.3 nmol/L to 1068.0 nmol/L, showing greater potency with longer 72 h incubation compared to 48 h incubation^[3].
HZX-02-059 (1 μmol/L; 12-24 h) induces prominent cytoplasmic vacuolization in Nalm6 and Sup-B15 B-ALL cells^[3].
HZX-02-059 (0.5-1.5 μmol/L; 24-48 h) induces dose- and time-dependent late apoptosis in Nalm6 and Sup-B15 B-ALL cells^[3].
HZX-02-059 (1 μmol/L; 24 h) alters transcriptome profiles in Nalm6 B-ALL cells, downregulating p53 and NF-κB pathways and upregulating apoptosis and cell cycle-related pathways^[3].
HZX-02-059 (0.5-1.5 μmol/L; 24 h) downregulates p53 signaling, PI3K/AKT signaling, and downstream c-Myc and NF-κB pathways in Nalm6 and Sup-B15 B-ALL cells, with concurrent changes in cell cycle-related protein expression^[3].
HZX-02-059 induces methuosis, inhibits proliferation, blocks cell cycle at G₂/M phase, and dysregulates the PI3K/AKT axis in B-cell acute lymphoblastic leukemia cell lines^[4].

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

Apoptosis Analysis^[2]

Cell Line:	Will-2, LR, and TMD8 DHL cell lines
Concentration:	0.25; 0.5; 1; 2; 4 μM
Incubation Time:	24; 48; 72 h
Result:	Induced a significant dose-dependent increase in dead (Annexin V+) cells, predominantly late apoptotic (Annexin V+/PI+) cells, and a corresponding decrease in live (Annexin V−/PI−) cells across all three DHL cell lines.

Cell Cycle Analysis^[2]

Cell Line:	Will-2, LR, and TMD8 DHL cell lines
Concentration:	0.5 μM
Incubation Time:	24 h
Result:	Caused a significant decrease in the percentage of cells in the S and G0/G1 phases, and a marked increase in the G2/M phase across all three DHL cell lines at 0.5 μM for 24 h.

Western Blot Analysis^[2]

Cell Line:	Will-2, LR, and TMD8 DHL cell lines
Concentration:	0.25; 0.5; 1 μM
Incubation Time:	24 h
Result:	Showed reduced α-tubulin, β-tubulin, phosphorylated mTOR, phosphorylated 4EBP1, and c-MYC expression, along with altered Cyclin B1 and CDC2 levels via western blot analysis, consistent with tubulin inhibition and mTOR/Myc axis suppression.

Apoptosis Analysis^[3]

Cell Line:	human B-cell acute lymphoblastic leukemia (B-ALL) cell lines Nalm6 and Sup-B15
Concentration:	0.5; 1; 1.5 μmol/L
Incubation Time:	24; 48 h
Result:	Triggered comparable levels of apoptosis in both cell lines after 24 h treatment with 1 or 1.5 μmol/L. Induced substantial apoptosis in both cell lines after 48 h treatment with all tested concentrations. Increased late apoptosis robustly, with no prominent increase in early apoptosis.

Western Blot Analysis^[3]

Cell Line:	human B-cell acute lymphoblastic leukemia (B-ALL) cell lines Nalm6 and Sup-B15
Concentration:	0.5; 1; 1.5 μmol/L
Incubation Time:	24 h
Result:	Decreased TP53, p27, CDC2, PI3K, phosphorylated AKT, c-Myc, and phosphorylated NF-κB p65 expression in a dose-dependent manner. Increased cyclin B1 expression. Decreased phosphorylated CDK2 expression. Left cyclin D1, cyclin B2, and total CDK2 expression unchanged.

In Vivo

HZX-02-059 (20 mg/kg; i.p.; daily; 7 days) significantly inhibits double-hit lymphoma xenograft growth in mice with no significant systemic toxicity^[2].

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

Animal Model:	NOD-Prkdc^−/−IL2rg^−/− (NPI) mice (female, 6 weeks old, double-hit lymphoma model via luciferase-labeled LR cells injection after 1 Gy irradiation)^[2]
Dosage:	20 mg/kg
Administration:	i.p.; daily; 7 consecutive days
Result:	Significantly inhibited tumor growth at day 12 compared to the vehicle group. Showed no statistically significant difference in average body mass compared to the vehicle group.

Molecular Weight

487.48

Formula

C₂₇H₂₀F₃N₅O

CAS No.

2240205-30-3

Appearance

Solid

Color

White to off-white

SMILES

CC(C=CC(NC(C1=CC(C(F)(F)F)=CC=C1)=O)=C2)=C2NC3=CC(C4=CN=CC=C4)=NC5=C3C=CN5

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 : 25 mg/mL (51.28 mM; ultrasonic and warming and adjust pH to 3 with HCl 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	2.0514 mL	10.2568 mL	20.5137 mL
5 mM	0.4103 mL	2.0514 mL	4.1027 mL
10 mM	0.2051 mL	1.0257 mL	2.0514 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

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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 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.13 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (4.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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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: 99.40%

Select Batch:

Data Sheet (286 KB) SDS (251 KB)

COA (251 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Roy A, et al. Selective Termination of Autophagy-Dependent Cancers. Cells. 2024 Jun 25;13(13):1096. [Content Brief]

[2]. Feng L, et al. Pharmacological targeting PIKfyve and tubulin as an effective treatment strategy for double-hit lymphoma. Cell Death Discov. 2022 Jan 28;8(1):39. [Content Brief]

[3]. Lu Z, et al. Novel PIKfyve/Tubulin Dual-target Inhibitor as a Promising Therapeutic Strategy for B-cell Acute Lymphoblastic Leukemia. Curr Med Sci. 2024 Apr;44(2):298-308. [Content Brief]

[4]. Zhen Lu, et al. An Azaindole-Based Small Molecule Hzx-02-059 Induces Methuosis in B-Cell Acute Lymphoblastic Leukemia through the PI3K/AKT Axis. Blood (2020) 136 (Supplement 1): 9.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0514 mL	10.2568 mL	20.5137 mL	51.2842 mL
	5 mM	0.4103 mL	2.0514 mL	4.1027 mL	10.2568 mL
	10 mM	0.2051 mL	1.0257 mL	2.0514 mL	5.1284 mL
	15 mM	0.1368 mL	0.6838 mL	1.3676 mL	3.4189 mL
	20 mM	0.1026 mL	0.5128 mL	1.0257 mL	2.5642 mL
	25 mM	0.0821 mL	0.4103 mL	0.8205 mL	2.0514 mL
	30 mM	0.0684 mL	0.3419 mL	0.6838 mL	1.7095 mL
	40 mM	0.0513 mL	0.2564 mL	0.5128 mL	1.2821 mL
	50 mM	0.0410 mL	0.2051 mL	0.4103 mL	1.0257 mL

HZX-02-059 Related Classifications

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HZX-02-059 (Synonyms: Methuosis inducer 1)

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HZX-02-059 (Synonyms: Methuosis inducer 1)

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