Art. -Nr.: HY-160237

HYL001

Name: HYL001
Brand: MedChemExpress
SKU: HY-160237
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HYL001 is an orally active, selective ALK4/ALK5 inhibitor with K_d values of 13 nM and 22.5 nM for ALK4 and ALK5, respectively. HYL001 inhibits GLS expression. HYL001 impairs glutamine metabolism, mitochondrial respiration, the TCA cycle, oxidative phosphorylation, ATP production, and redox balance, while selectively targeting mitochondria, disrupting mitochondrial structure, and inducing Apoptosis and ROS. HYL001 inhibits tumor growth and liver metastasis. HYL001 can be used in research on breast cancer, hepatocellular carcinoma, and microsatellite-stable colorectal cancer metastasis.

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Reinheit : 99.94%
CAS. Nr.: 2426547-83-1
Formel: C₂₁H₁₈N₄O
Molecular Weight:342.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

HYL001 Chemical Structure

CAS. Nr.: 2426547-83-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

TGFβ^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
H22	IC50	1.4 μM	Cytotoxicity against murine H22 hepatocellular carcinoma cells with IC50 1.4 µM. Cytotoxicity against murine H22 hepatocellular carcinoma cells with IC50 1.4 µM.	36958408
HEK-293T	IC50	72 nM	Inhibition of TGFβ pathway activity in HEK293T cells transfected with 12xCAGA-Firefly_Luc and Tk-Renilla_Luc reporters incubated 16 hrs with 5 ng/mL TGFB1 measured by dual luciferase assay. Inhibition of TGFβ pathway activity in HEK293T cells transfected with 12xCAGA-Firefly_Luc and Tk-Renilla_Luc reporters incubated 16 hrs with 5 ng/mL TGFB1 measured by dual luciferase assay.	39816803

In Vitro

Protein/Amino Acid MetabolismAnti-cancerMitochondrial FunctionApoptosisOxidative StressBacterial InfectionOthers

Protein/Amino Acid Metabolism

HYL001 downregulates GLS expression in 4T1 breast cancer cells^[1].
HYL001 exhibits marginal inhibitory activity against purified recombinant GLS^[2].

Anti-cancer

HYL001 displayed IC₅₀ >20 µM in normal NIH-3T3 and HUVEC cells, and IC₅₀ <5 µM in tumor cells^[2].
HYL001 (1-10 µM) inhibited 4T1 TRC colony formation, with 100% inhibition at 10 µM, and inhibited preformed 4T1 TRC colonies by 60% at 10 µM^[2].
HYL001 (1-10 µM) inhibits HCSC with an IC₅₀ 340-fold lower than that of LND, and inhibits H22 TRC colony growth at 1 µM, with an inhibition rate of 58% at 10 µM^[2].
HYL001 inhibits breast CSC and HCC stem cells, with IC₅₀ values 380-fold and 340-fold lower than Lonidamine (HY-B0486), respectively^[4].

Anti-cancer

Mitochondrial Function

HYL001 (1 µM; 12 h) damaged the mitochondria of nearly 100% of BCSCs^[2].
HYL001 (5 µM; 12 h) reduced ATP in BCSCs by nearly 100%^[2].

Anti-cancer

Apoptosis

HYL001 (1-5 µM; 12 h) induced apoptosis in BCSCs, with apoptosis rates of 30%, 32%, and 55%, respectively^[2].

Anti-cancer

Protein/Amino Acid Metabolism

HYL001 (1 µM; 12 h) increases Gln and inhibits the Glu/Gln ratio in BCSCs^[2].

Anti-cancer

Oxidative Stress

Mitochondrial Function

HYL001 (1-5 µM; 4 h) enhances mitochondrial ROS in BCSCs, with a 3-fold increase at 5 µM^[2].

Oxidative Stress

Anti-cancer

HYL001 inhibits GLS, reduces GSH, enhances ROS, and impairs the TCA cycle/OXPHOS in 4T1 and H22 cancer cells^[4].

Bacterial Infection

HYL001 (1-320 µg/mL) showed no mutagenic potential in S. typhimurium strains TA98, TA100, TA1535, and TA1537 with or without S9^[7].

Others

HYL001 (0.3-10 μM) is a potent ALK4/ALK5 inhibitor with a K_d of 22.5 nM for ALK5, and shows limited off-target binding at 300 nM, primarily binding to p38α^[5].
HYL001 (0.1-10,000 nM; 16 hours) inhibits TGFβ pathway activity in HEK293T reporter cells with an IC₅₀ of 72 nM^[5].
HYL001 is a potent inhibitor of ALK4 and ALK5, with K_d values of 13 nM and 22.5 nM, respectively, in cell-free competitive binding assays^[7].
HYL001 inhibited ALK5 with an IC₅₀ of 177 nM and p38α with an IC₅₀ of 548 nM in recombinant kinase activity assays^[7].

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

Apoptosis Analysis^[2]

Cell Line:

BCSCs
Concentration:

1, 3, 5 µM
Incubation Time:

12 h
Result:

The apoptosis rate of BCSCs was 30%, 32%, and 55% after HYL001 exposure at 1 µM, 3 µM, and 5 µM for 12 h, respectively.

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_last	AUC_inf	T_1/2	CL/F
Mice^[5]	71 mg/kg	p.o.	0.25 h	2050 ng/mL	3520 ng·h/mL	4110 ng·h/mL	2.45 h	288 mL/min/kg

In Vivo

Anti-cancerProtein/Amino Acid Metabolism

Anti-cancer

HYL001 (5 μmol/kg; s.c.; once every three days; five injections) inhibits subcutaneous 4T1 tumor growth and reduces breast cancer stem cell populations in BALB/c mice^[2].
HYL001 (5 μmol/kg; s.c.; once every three days; five injections) suppresses lung metastasis and prolongs survival in the metastatic 4T1 tumor model in BALB/c mice^[2].

Anti-cancer

Protein/Amino Acid Metabolism

HYL001 (10 μmol/kg; 10 μmol/kg plus PTX 20 μmol/kg; i.v.; once every three days; five times) inhibits orthotopic 4T1 tumor growth, blocks glutamine metabolism, and reduces cancer stem cell populations in BALB/c mice^[2].
HYL001 (10 μmol/kg; i.v.; every 2 days; 5 doses) inhibits orthotopic 4T1 tumor growth in female BALB/c mice, with ~28% tumor inhibition by weight, ~57% reduction in intratumoral Glu/Gln ratio, reduced GLS expression, and decreased CD133 CSC staining^[6].

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

Animal Model:

BALB/c (female, five-week-old)^[2]
Dosage:

5 μmol/kg
Administration:

s.c.; once every three days; five injections
Result:

Inhibited tumor growth with a tumor inhibition rate (TIR) of 44% in tumor volume.
Reduced the proportion of CD133+ cancer cells by 82.1%, side population cells by 62.1%, and CD44+CD24− cancer cells by 38.2% relative to saline.
The G0/G1 ratio of CD133+ cancer cells declined from 90% to 70%.
Enhanced ROS and reduced GSH in subcutaneous 4T1 tumor tissues.

Animal Model:

BALB/c (female, five-week-old)^[2]
Dosage:

5 μmol/kg
Administration:

s.c.; once every three days; five injections
Result:

Reduced pulmonary metastatic nodules from nearly 300 in the saline group to 60.
Overall survival was prolonged by 10 days (31.2%) over the saline group.
Circulating tumor cells and circulating tumor stem cells were significantly lower in mice given HYL001 than in saline or LND groups.
Greater reduction was noted in circulating tumor stem cells than in circulating tumor cells after HYL001 administration.
Lung wet weight was mildest in the HYL001 group.

Animal Model:

BALB/c (female, five-week-old)^[2]
Dosage:

10 μmol/kg (monotherapy); 10 μmol/kg plus PTX 20 μmol/kg
Administration:

i.v.; once every three days; five times
Result:

Monotherapy achieved a tumor inhibition rate (TIR) of 36%.
HYL001 plus PTX achieved a TIR of 75%.
Relative Glu/Gln values were reduced to 49% after HYL001 administration and to 31% after HYL001 plus PTX administration relative to saline.
Decreased GSH and enhanced mitochondrial ROS in orthotopic 4T1 tumor tissues.
Significantly reduced CD133+ cells, with green fluorescence intensity declining by around 90%.
CSC populations including CD133+ cells, CD44+CD24− cells, and side population cells were decreased in tumors from mice given HYL001.

Animal Model:

BALB/c (female, SPF, 16-20 g)^[6]
Dosage:

10 μmol/kg
Administration:

i.v.; once every 2 days; 5 doses
Result:

Tumor inhibition rate by weight was ~28% in the HYL001 group.
Intratumoral Glu/Gln ratio was reduced by ~57% in the free HYL001 group compared with Saline.
GLS expression was drastically reduced in orthotopic 4T1 tumor tissues upon administration of free HYL001.
CD133 fluorescence staining confirmed that HYL001 administration declined CSCs in orthotopic 4T1 tumor tissues.

Related Protocols :

Chemical Information

CAS. Nr. 2426547-83-1
Appearance Solid
Molecular Weight 342.39
Formel C₂₁H₁₈N₄O
Color White to off-white
SMILES

OC1=CC2=C(C3=C(CCC4)N4N=C3C5=CC=CC(C)=N5)C=CN=C2C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 17.5 mg/mL (51.11 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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9206 mL

14.6032 mL

29.2065 mL

5 mM

0.5841 mL

2.9206 mL

5.8413 mL

10 mM

0.2921 mL

1.4603 mL

2.9206 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (301 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zou W, et al. Targeting glutamine metabolism as a potential target for cancer treatment. Journal of experimental & clinical cancer research : CR. 2025 Jul 01;44(1):180.

[2]. Wang Q, et al. A novel lonidamine derivative targeting mitochondria to eliminate cancer stem cells by blocking glutamine metabolism. Pharmacological research. 2023 Apr;190:106740.

[3]. Fan Z, et al. Boosting oxidative stress with hydroxyethyl starch smart nanomedicines to eliminate cancer stem cells. Accounts of Materials Research. 2024 Oct 24;5(12):1558-70.

[4]. De Los Santos-Jiménez J, et al. GLS and GLS2 Glutaminase Isoenzymes in the Antioxidant System of Cancer Cells. Antioxidants (Basel, Switzerland). 2024 Jun 20;13(6):745.

[5]. Tauriello DVF, et al. New Potent Inhibitor of Transforming Growth Factor-Beta (TGFβ) Signaling that is Efficacious against Microsatellite Stable Colorectal Cancer Metastasis in Combination with Immune Checkpoint Therapy in Mice. ACS pharmacology & translational science. 2025 Jan 10;8(1):97-112.

[6]. Wang Q, et al. Glutaminolysis inhibition boosts photodynamic therapy to eliminate cancer stem cells. Biomaterials. 2024 Apr;306:122497. [Content Brief]

[7]. Tauriello DV, et al. HYL001, a new potent TGFβ signaling inhibitor that is efficacious against microsatellite stable CRC metastasis in combination with immune checkpoint therapy in mice. bioRxiv. 2024 May 14:2024-05.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.9206 mL	14.6032 mL	29.2065 mL	73.0161 mL
	5 mM	0.5841 mL	2.9206 mL	5.8413 mL	14.6032 mL
	10 mM	0.2921 mL	1.4603 mL	2.9206 mL	7.3016 mL
	15 mM	0.1947 mL	0.9735 mL	1.9471 mL	4.8677 mL
	20 mM	0.1460 mL	0.7302 mL	1.4603 mL	3.6508 mL
	25 mM	0.1168 mL	0.5841 mL	1.1683 mL	2.9206 mL
	30 mM	0.0974 mL	0.4868 mL	0.9735 mL	2.4339 mL
	40 mM	0.0730 mL	0.3651 mL	0.7302 mL	1.8254 mL
	50 mM	0.0584 mL	0.2921 mL	0.5841 mL	1.4603 mL

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HYL001