Referencia número: HY-100957A

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Dilazep

Name: Dilazep
Brand: MedChemExpress
SKU: HY-100957A
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2 Cited Publications

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Dilazep is a GATA2 inhibitor and an hENT1-mediated nucleoside transport inhibitor. Dilazep acts by blocking GATA2 chromatin recruitment and DNA binding, reducing GATA2 thermal stability, and inhibiting AR, c-MYC, the cell cycle, DNA replication/repair, and metastatic transcriptional programs; it also inhibits Adenosine (HY-B0228) reuptake and cardiac adenosine uptake, enhancing adenosine-induced coronary vasodilation. Dilazep can be used in research on atherosclerosis, ischemic heart disease, and castration-resistant prostate cancer.

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No. CAS: 35898-87-4
Fòrmula: C₃₁H₄₄N₂O₁₀
Peso molecular:604.69

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Dilazep Chemical Structure

No. CAS: 35898-87-4

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Cell Proliferation/Viability AssayCell Imaging/Staining

Cell Imaging/Staining
Cell Proliferation/Viability Assay
Cell Proliferation/Viability Assay
Cell Proliferation/Viability Assay
Cell Proliferation/Viability Assay

Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
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Actividad biológica

Descripciòn

Cellular Effect

Cell Line	Type	Value	Description	References
Erythrocyte	IC50	≈ 7 nM	Inhibition of [³H]uridine equilibrium exchange in human erythrocytes using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine equilibrium exchange in human erythrocytes using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
Erythrocyte	IC50	≈ 40 nM	Inhibition of [³H]uridine equilibrium exchange in mouse erythrocytes using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine equilibrium exchange in mouse erythrocytes using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
Erythrocyte	IC50	≈ 1000 nM	Inhibition of [³H]uridine equilibrium exchange in rat erythrocytes using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine equilibrium exchange in rat erythrocytes using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
HeLa	IC50	5 nM	Inhibition of [³H]uridine zero-trans influx in human HeLa cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay, high-sensitivity component. Inhibition of [³H]uridine zero-trans influx in human HeLa cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay, high-sensitivity component.	3349106
HeLa	IC50	3000 nM	Biphasic inhibition of [³H]uridine zero-trans influx in human HeLa cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay, low-sensitivity component. Biphasic inhibition of [³H]uridine zero-trans influx in human HeLa cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay, low-sensitivity component.	3349106
HEp-2	IC50	≈ 5 nM	Inhibition of [³H]uridine zero-trans influx in human Hep-2 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine zero-trans influx in human Hep-2 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
L1210	IC50	≈ 30 nM	Inhibition of [³H]uridine zero-trans influx in mouse L1210 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine zero-trans influx in mouse L1210 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
P388	IC50	≈ 10 nM	Inhibition of [³H]uridine zero-trans influx in mouse P388 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine zero-trans influx in mouse P388 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
S49	IC50	≈ 10 nM	Inhibition of [³H]uridine zero-trans influx in mouse S49 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine zero-trans influx in mouse S49 cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
W256	IC50	> 10000 nM	Inhibition of [³H]uridine zero-trans influx in rat Walker 256 carcinoma cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay, with IC₅₀ greater than 10000 nM. Inhibition of [³H]uridine zero-trans influx in rat Walker 256 carcinoma cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay, with IC₅₀ greater than 10000 nM.	3349106
NRK	IC50	400 nM	Inhibition of [³H]uridine zero-trans influx in rat NRK cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine zero-trans influx in rat NRK cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106
CHO	IC50	1000 nM	Inhibition of [³H]uridine zero-trans influx in hamster CHO cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay. Inhibition of [³H]uridine zero-trans influx in hamster CHO cells using 500 μM substrate after at least 5 min preincubation by rapid kinetic transport assay.	3349106

In Vitro

Anti-cancerCell Cycle RegulationNucleotide MetabolismCardiovascular RegulationRegulation of Cardiac Pump FunctionLipid MetabolismLocal Vascular RegulationMitochondrial FunctionCarbohydrate MetabolismOthers

Anti-cancer

Dilazep (50-100 µM; 16 hours) reduces GATA2 DNA binding in LNCaP nuclear extracts^[6].
Dilazep (96 hours) inhibits the viability of GATA2-dependent LNCaP, LAPC4, Abl, 22Rv1, and MDVR prostate cancer cells, with lower activity in PC-3 and RWPE-1 cells^[6].

Anti-cancer

Cell Cycle Regulation

Nucleotide Metabolism

Dilazep (50 µM; 48 hours) inhibits GATA2-, AR-, c-MYC-, cell cycle-, DNA repair-, stemness-, and metastasis-related transcriptional programs in LNCaP, Abl, and MDVR cells^[6].

Cardiovascular Regulation

Regulation of Cardiac Pump Function

Dilazep (1-10 μM; from 5 minutes before ischemia to the end of 15-minute ischemia) reduces pre-ischemic RPP at 5 and 10 μM in isolated working rat hearts, but has no such effect at 1 μM, does not alter coronary flow, and improves post-ischemic recovery of RPP and coronary flow after 15-minute ischemia and 20-minute reperfusion^[5].

Cell Cycle Regulation

Dilazep (20-50 µM; 24 hours) reduces S-phase entry in 22Rv1 and LNCaP cells^[6].

Lipid Metabolism

Dilazep (1-10 μM; from 5 minutes before ischemia to the end of 15 minutes of ischemia) attenuates reperfusion-induced free fatty acid accumulation at 1, 5, and 10 μM in isolated working rat hearts, with 10 μM also reducing post-ischemic arachidonic acid (HY-109590)^[5].

Local Vascular Regulation

Dilazep (100 μM; 10 minutes to 24 hours) suppresses PpET-1 transcription to 0.04 normalized units at 24 h in subconfluent serum-treated BAEC and suppresses ET-1 peptide release to 38.8 pg/mL at 24 h^[3].
Dilazep (12-24 hours) suppresses PpET-1 transcription to 0.47 at 12 hours in confluent serum-treated BAEC and suppresses ET-1 peptide release to 955.5 pg/mL at 12 hours^[3].
Dilazep (1-100 μM; 16 hours) inhibits PpET-1 transcription in serum-treated BAEC in a concentration-dependent manner, reaching 0.42 at 100 μM after 16 hours^[3].
Dilazep (100 μM; 3-6 hours) inhibits PpET-1 transcription to 0.41 at 3 hours and ET-1 peptide release to 299.0 pg/mL at 3 hours in serum-treated HUVECs^[3].
Dilazep (100 μM; 0-4 hours) suppresses PpET-1 transcription to 0.30 at 1 hour and 0.08 at 2 hours in serum-deprived BAEC stimulated with Thrombin (MW 37kDa) (HY-114164)^[3].
Dilazep (100 μM; 24 hours) inhibits ET-1 promoter activity by 99% at 24 hours in BAEC transfected with the 5-kb ET-1 promoter-luciferase construct^[3].

Mitochondrial Function

Carbohydrate Metabolism

Nucleotide Metabolism

Dilazep (1-10 μM; from 5 minutes before ischemia to the end of 15 minutes of ischemia) preserves ATP and CrP and reduces Lactic acid (HY-B2227) at 5 and 10 μM, but not at 1 μM, in isolated working rat hearts after 15 minutes of ischemia and 20 minutes of reperfusion^[5].

Nucleotide Metabolism

Dilazep (1 nM-100 μM; ≥ 5 minutes) inhibits Uridine (HY-B1449) equilibrium exchange in erythrocytes, with an IC₅₀ ≈ 7 nM in human erythrocytes, ≈ 20 nM in porcine erythrocytes, ≈ 30 nM in rabbit erythrocytes, ≈ 40 nM in mouse erythrocytes, and ≈ 1000 nM in rat erythrocytes^[4].
Dilazep (50 µM; 48 hours) reduces AR, c-MYC, EZH2, RRM2, phosphorylated Rb, BRCA1, and CHK2 protein levels in LNCaP, Abl, and MDVR cells^[6].

Nucleotide Metabolism

Anti-cancer

Dilazep (1 nM-100 μM; ≥ 5 min) inhibits zero-trans influx of uridine in cultured cells, with IC₅₀ ≈ 5 nM in Hep-2, 5/3000 nM in HeLa, ≈ 10-30 nM in mouse L1210/P388/S49, ≈ 400 to >10000 nM in rat NRK/HTC/Novikoff/Walker 256, 20 nM in BHK, and 1000 nM in CHO cells^[4].

Others

Dilazep (10-50 µM; 72 hours) reduces AR and c-MYC protein levels in LNCaP, 22Rv1, and LAPC4 cells^[6].
Dilazep (50 µM; 1 hour) binds to GATA2 in 22Rv1 cells, producing thermal destabilization with a T_m of 64-67°C^[6].
Dilazep (10 µM; 16 hours) reduces GATA2 occupancy at the KLK3/PSA and c-MYC loci in LNCaP cells without reducing GATA2 protein^[6].
Dilazep (10 µM; 24 hours) reduces GATA2-dependent PSA/KLK3 reporter activity in 22Rv1 cells^[6].
Dilazep (10 μM; 4 days) blocks adenosine-rescued growth of wild-type hENT1 in hENT1-expressing W303-1A yeast, but has no such effect on the L92P mutant^[7].
Dilazep (0.01-1000 nM; 20-minute preincubation, 20-minute uptake) inhibits [³H]adenosine transport, with an IC₅₀ of 0.74 nM for wild-type hENT1 and an IC₅₀ of 2.8 nM for L92Q in hENT1-expressing YPL1 yeast^[7].

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

Cell Proliferation Assay^[6]

Cell Line:

22Rv1 and LNCaP cells
Concentration:

20 and 50 µM
Incubation Time:

24 h
Result:

Caused concentration-dependent reduction in the percentage of S-phase cells in 22Rv1 and LNCaP cells.

Western Blot Analysis^[6]

Cell Line:

LNCaP, 22Rv1, and LAPC4 cells
Concentration:

10, 20, and 50 µM
Incubation Time:

72 h
Result:

AR and c-MYC protein levels decreased dose-dependently in LNCaP, 22Rv1, and LAPC4 cells.
AR-V7 was also decreased in 22Rv1 cells.

In Vivo

Anti-cancer

Dilazep (50 mg/kg; i.p.; daily 5 days per week (Monday-Friday)) inhibits MDA-PCa-337A castration-resistant prostate cancer PDX tumor growth in castrated SCID mice without causing body-weight loss^[6].

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

Animal Model:

CB17SCID (CB17/Icr-Prkdcscid/IcrIcoCrl; male; six weeks old)^[6]
Dosage:

50 mg/kg
Administration:

i.p.; daily 5 days per week (Monday-Friday); initiated one day after implantation
Result:

Inhibited MDA-PCa-337A PDX tumor growth.
No loss of animal body weight was observed.

Related Protocols :

Chemical Information

No. CAS 35898-87-4
Peso molecular 604.69
Fòrmula C₃₁H₄₄N₂O₁₀
SMILES

O=C(C1=CC(OC)=C(OC)C(OC)=C1)OCCCN2CCN(CCCOC(C3=CC(OC)=C(OC)C(OC)=C3)=O)CCC2
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Publications (2)

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bioRxiv

2025 Oct 23.

Dilazep purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 23.

Cell numbers were measured using the CyQUANT assay after 12 days culture in glutamine-deprived medium supplemented with 1 mM α-KG and 2.5 µM exDNA, with or without co-treatment using nucleoside transporter inhibitors (NBTI, DPL, or Dilazep dihydrochloride) at 0.01 µM (+), 0.1 µM (++), or 1 µM (+++).

Dilazep purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 23.

Cell numbers were measured using the CyQUANT assay after 12 days culture in glutamine-deprived medium supplemented with 1 mM α-KG and 2.5 µM exDNA, with or without co-treatment using nucleoside transporter inhibitors (NBTI, DPL, or Dilazep dihydrochloride) at 0.01 µM (+), 0.1 µM (++), or 1 µM (+++).

Dilazep purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 23.

Cell numbers were measured using the CyQUANT assay after 12 days culture in glutamine-deprived medium supplemented with 1 mM α-KG and 2.5 µM exDNA, with or without co-treatment using nucleoside transporter inhibitors (NBTI, DPL, or Dilazep dihydrochloride) at 0.01 µM (+), 0.1 µM (++), or 1 µM (+++).

Dilazep purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Oct 23.

Cell numbers were measured using the CyQUANT assay after 12 days culture in glutamine-deprived medium supplemented with 1 mM α-KG and 2.5 µM exDNA, with or without co-treatment using nucleoside transporter inhibitors (NBTI, DPL, or Dilazep dihydrochloride) at 0.01 µM (+), 0.1 µM (++), or 1 µM (+++).
bioRxiv

2025 Sep 4.

Dilazep purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 Sep 4.

Representative images of WT Hela cells or VPS13B KO cells treated with: azelastine (AZL); Dilazep dihydrochloride (DLZ). 10 µM, 24 h. cells were fixed and stained with an anti-LBPA antibody (upper panel) of with Filipin (lower panel).

Pureza y Documentación

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Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (285 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Telesnicki K. Assessing the impact of GATA2 inhibition on macrophage atherogenic activity (Doctoral dissertation, et al.

[2]. Marzilli M, et al. Effects of dilazep on coronary and systemic hemodynamics in humans. American heart journal. 1984 Aug;108(2):276-85.

[3]. Shrestha B, et al. Endothelin-1 gene expression in endothelial cells is potently inhibited by a vasodilator, dilazep. Hypertension research : official journal of the Japanese Society of Hypertension. 2004 Jun;27(6):409-15.

[4]. Plagemann PG, et al. Species differences in sensitivity of nucleoside transport in erythrocytes and cultured cells to inhibition by nitrobenzylthioinosine, dipyridamole, dilazep and lidoflazine. Biochimica et biophysica acta. 1988 Apr 02;969(1):1-8.

[5]. Hoque AN, et al. A study on dilazep: I. Mechanism of anti-ischemic action of dilazep is not coronary vasodilation but decreased cardiac mechanical function in the isolated, working rat heart. Japanese journal of pharmacology. 1995 Mar;67(3):225-32.

[6]. Kaochar S, et al. Inhibition of GATA2 in prostate cancer by a clinically available small molecule. Endocrine-related cancer. 2021 Nov 24;29(1):15-31.

[7]. Endres CJ, et al. Mutation of leucine-92 selectively reduces the apparent affinity of inosine, guanosine, NBMPR [S6-(4-nitrobenzyl)-mercaptopurine riboside] and dilazep for the human equilibrative nucleoside transporter, hENT1. The Biochemical journal. 2004 May 15;380(Pt 1):131-7. [Content Brief]

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Dilazep

Publications Citing Use of MedChemExpress (MCE) Dilazep

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Chemical Information

Publications (2)

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