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Cat. No.: HY-190906

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JH-1

JH-1 is an orally active and selective KDM1A inhibitor (IC₅₀ = 0.035 μM). JH-1 reversibly inhibits KDM1A and blocks histone demethylation; it binds KDM1A intracellularly and elevates H3K4me1/2 methylation levels in a dose-dependent manner. JH-1 induces ferroptosis and apoptosis in esophageal cancer cells, upregulates ACSL4, BAX, and Cleaved‑caspase‑3, downregulates GPX4 and Bcl‑2, and increases ROS and MDA. JH-1 inhibits tumor growth and upregulates ferroptosis and apoptosis markers in the KYSE510 esophageal cancer xenograft model. JH-1 can be used for research related to esophageal cancer.

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CAS No.: 3128804-75-8
화학식: C₂₄H₂₄N₄O
분자량:384.47

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

JH-1 Chemical Structure

CAS No.: 3128804-75-8

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

Caspase 3

Bax

Bcl-2

GPX4

ACSL4

All Histone Demethylase Isoforms :

All Caspase Isoforms :

All Glutathione Peroxidase Isoforms :

GPX1
GPX4

All ACSL Family Isoforms :

ACSL4
ACSL5

All Bcl-2 Family Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KYSE-510	IC50	5.86 μM	Cytotoxicity against human KYSE510 esophageal cancer cells assessed as viability reduction incubated 5 days by CCK-8 assay. Cytotoxicity against human KYSE510 esophageal cancer cells assessed as viability reduction incubated 5 days by CCK-8 assay.	acs.jmedchem.6c01218
HET-1A	IC50	23.24 μM	Cytotoxicity against human HET-1A normal esophageal epithelial cells assessed as viability reduction incubated 5 days by CCK-8 assay. Cytotoxicity against human HET-1A normal esophageal epithelial cells assessed as viability reduction incubated 5 days by CCK-8 assay.	acs.jmedchem.6c01218

In Vitro

Anti-cancerApoptosisFerroptosisOxidative StressOthers

Anti-cancer

JH-1 (6 h) binds KDM1A at the cellular level in KYSE510 cells^[1].
JH-1 (0.5-4 μM; 5 days) inhibits KDM1A demethylase activity in KYSE510 cells, increases H3K4me1/2 without affecting H3K4me3; promotes the ferroptosis-related protein profile and activates intrinsic apoptosis markers in KYSE510 cells; the mediated changes in histone methylation depend on KDM1A^[1].
JH-1 (5 days) selectively reduces KYSE510 cell viability compared with HET-1A cells, with KYSE510 IC₅₀ = 5.86 μM and HET-1A IC₅₀ = 23.24 μM^[1].
JH-1 (0.5-4 μM; 7 days) inhibits clonogenic growth of KYSE510 cells^[1].

Anti-cancer

Apoptosis

JH-1 (0.5-4 μM; 5 days) induces dose-dependent apoptosis in KYSE510 cells, and the induced apoptosis largely depends on KDM1A^[1].

Anti-cancer

Apoptosis

Ferroptosis

JH-1 (2 μM; 5 days) combined with Fer-1 and Z-VAD-FMK (HY-16658B): both ferroptosis and apoptosis are involved in JH-1-induced KYSE510 cell death^[1].

Anti-cancer

Ferroptosis

JH-1 (2 μM) combined with Fer-1 (HY-100579) (2 μM) rescues JH-1-induced changes in ferroptosis-related proteins in KYSE510 cells^[1].

Oxidative Stress

Anti-cancer

JH-1 (0.5-4 μM) disrupts the redox balance in KYSE510 cells by decreasing GSH/GSSG; the induced glutathione redox imbalance in KYSE510 cells largely depends on KDM1A^[1].

Oxidative Stress

Anti-cancer

Ferroptosis

JH-1 (0.5-4 μM; 5 days) induces dose-dependent lipid ROS accumulation in KYSE510 cells, and this effect is significantly attenuated in KDM1A KO KYSE510 cells^[1].

Others

JH-1 is a potent cell-free KDM1A inhibitor with an IC₅₀ of 35 nM and exhibits selectivity for KDM1A over LSD2, MAO-A, and MAO-B^[1].

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

Western Blot Analysis^[1]

Cell Line:

KYSE510 cells, KYSE510 KDM1A knockout cells
Concentration:

0.5, 1, 2, and 4 μM
Incubation Time:

5 days
Result:

Upregulated ACSL4 and downregulated GPX4. Upregulated cleaved-caspase3, cleaved-PARP1, Bax, and P53, and downregulated PARP1 and pro-caspase3.
Did not change KDM1A expression; H3K4me1 and H3K4me2 levels increased in a dose-dependent manner; H3K4me3 was unaffected.
Had no effect on H3K4me1, H3K4me2, or H3K4me3 methylation in KDM1A KO cells.

Cell Proliferation Assay^[1]

Cell Line:

KYSE510 cells
Concentration:

0.5, 1, 2, and 4 μM
Incubation Time:

7 days
Result:

Inhibited KYSE510 colony formation.

Apoptosis Analysis^[1]

Cell Line:

KYSE510 cells
Concentration:

0.5, 1, 2, and 4 μM
Incubation Time:

5 days
Result:

Induced dose-dependent apoptosis in KYSE510 cells, and the induced apoptosis largely depends on KDM1A.

Cell Viability Assay^[1]

Cell Line:

KYSE510 cells
Concentration:

2 μM
2 μM (Fer-1); 2 μM (Z-VAD-FMK)
Incubation Time:

5 days
Result:

Reduced KYSE510 survival, and both Fer-1 and Z-VAD-FMK significantly alleviated cell death.

Parmacokinetics

Species	Dose	Route	T_max	C_max	T_1/2	MRT_0-inf	AUC_0-last	AUC_inf
Mice^[1]	40 mg/kg	p.o.	0.42 h	422 ng/mL	0.95 h	1.65 h	925 ng·h/mL	930 ng·h/mL

In Vivo

Anti-cancerFerroptosisApoptosisOxidative Stress

Anti-cancer

Ferroptosis

Apoptosis

Oxidative Stress

JH-1 (10-40 mg/kg/day; p.o.; daily; 2 weeks) inhibits the growth of KYSE510 esophageal cancer xenograft tumors and induces changes in intratumoral ferroptosis- and apoptosis-related biomarkers^[1].

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

Animal Model:

BALB/c-nu (female, 5-6 weeks old, 18-20 g, 1 × 10⁷ KYSE510 cells were subcutaneously injected into the right axillary region)^[1]
Dosage:

10 mg/kg/day; 20 mg/kg/day; 40 mg/kg/day
Administration:

p.o.; daily; 2 weeks
Result:

Suppressed KYSE510 xenograft tumor growth, with reduced tumor volume during the 2-week administration period and decreased tumor weight in the 10, 20, and 40 mg/kg/day groups compared with vehicle.
Promoted lipid ROS accumulation in tumor tissues in a dose-dependent manner.
Increased intratumoral ACSL4 and BAX protein expression and decreased GPX4 expression; immunohistochemistry showed increased cleaved-caspase3 in tumor tissues.

Related Protocols :

Chemical Information

CAS No. 3128804-75-8
분자량 384.47
화학식 C₂₄H₂₄N₄O
SMILES

OC(C=C1)=CC=C1C2=CC=C3C(N=CN=C3NC4=CC=C(N(CC)CC)C=C4)=C2
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Zhao L J, et al. Discovery of Novel Quinazoline-Based KDM1A Inhibitors as Dual Inducers of Ferroptosis and Apoptosis in Esophageal Cancer. Journal of Medicinal Chemistry, 2026.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
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상품명:
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수량:

JH-1

All Histone Demethylase Isoforms

All Caspase Isoforms

All Glutathione Peroxidase Isoforms

All ACSL Family Isoforms

All Bcl-2 Family Isoforms