2. Apoptosis Autophagy
  3. Caspase Apoptosis Autophagy Necroptosis
  4. Z-VAD

Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation.

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

Z-VAD Chemical Structure

Z-VAD Chemical Structure

CAS No. : 162852-62-2

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Based on 4 publication(s) in Google Scholar

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Description

Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation[1].

IC50 & Target

Caspase 3

 

Caspase-6

 

Caspase-7

 

Caspase-8

 

Caspase-9

 

In Vitro

Z-VAD (50 μM; 24 h) enhances the sensitivity of MDA-MB-231 breast cancer cells and H460 lung cancer cells to ionizing radiation[1].
Z-VAD (50 μM; 24h, 48h) combined with radiotherapy induces increasing autophagosome formation in breast cancer and lung cancer cells and upregulated the expression of autophagy-related proteins such as ATG5-ATG12 complex and Beclin-1[1].
Z-VAD (50 μM) combined with radiotherapy significantly reduces the formation of capillary-like tube structures in human umbilical vein endothelial cells (HUVECs)[1].

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

Cell Viability Assay[1]

Cell Line: MDA-MB-231 (breast cancer), H460 (lung cancer)
Concentration: 50 μM
Incubation Time: 24 h; followed by irradiation (0-6 Gy)
Result: Significantly reduced the surviving fraction of both cell lines, with a dose enhancement ratio (DER) of 1.31, indicating increased radiosensitivity compared to radiation alone.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 (breast cancer), H460 (lung cancer)
Concentration: 50 μM
Incubation Time: 24 h (GFP-LC3 imaging), 24 h/48 h (Western blotting); combined with 5 Gy radiation
Result: Significantly increased punctate autophagosome formation, compared to single treatments.
Upregulated the expression of ATG5-ATG12 complex and Beclin-1 proteins at 24 h and 48 h after combined treatment, indicating induction of autophagy-related pathways.

Cell Migration Assay [1]

Cell Line: HUVECs (human umbilical vein endothelial cells)
Concentration: 50 μM
Incubation Time: Pre-treatment for 24 h before seeding on Matrigel
Result: Significantly decreased the number of capillary-like tubules formed by HUVECs on Matrigel, with an average reduction from 47.66 (control) to 6.0 tubules per microscopic field, demonstrating anti-angiogenic effects.
In Vivo

Z-VAD (5 mg/kg; intraperitoneal injection; three times a week; 4 weeks) significantly inhibits tumor growth in nude mouse MDA-MB-231 breast cancer and H460 lung cancer xenograft tumor models when combined with radiotherapy and was well tolerated[1].

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

Animal Model: Female BALB/c nude mice (6-8 weeks old, 18-22 g) bearing MDA-MB-231 breast cancer or H460 lung cancer xenograft tumors[1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, three times a week, for 4 weeks
Result: Treatment with 5 mg/kg Z-VAD via intraperitoneal injection three times a week for 4 weeks, combined with radiotherapy, significantly reduced the tumor volume in both MDA-MB-231 and H460 xenograft models compared to radiotherapy alone.
The mice showed no significant signs of toxicity or adverse effects, indicating good tolerance to the treatment.
Molecular Weight

437.44

Formula

C20H27N3O8
CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Z-Val-Ala-Asp
Sequence Shortening

Z-VAD
SMILES

OC(C[C@@H](C(O)=O)NC([C@H](C)NC([C@H](C(C)C)NC(OCC1=CC=CC=C1)=O)=O)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (114.30 mM; Need ultrasonic; 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 2.2860 mL 11.4301 mL 22.8603 mL
5 mM 0.4572 mL 2.2860 mL 4.5721 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Number of animals

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

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 (sealed storage, away from moisture). 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 2.2860 mL 11.4301 mL 22.8603 mL 57.1507 mL
5 mM 0.4572 mL 2.2860 mL 4.5721 mL 11.4301 mL
10 mM 0.2286 mL 1.1430 mL 2.2860 mL 5.7151 mL
15 mM 0.1524 mL 0.7620 mL 1.5240 mL 3.8100 mL
20 mM 0.1143 mL 0.5715 mL 1.1430 mL 2.8575 mL
25 mM 0.0914 mL 0.4572 mL 0.9144 mL 2.2860 mL
30 mM 0.0762 mL 0.3810 mL 0.7620 mL 1.9050 mL
40 mM 0.0572 mL 0.2858 mL 0.5715 mL 1.4288 mL
50 mM 0.0457 mL 0.2286 mL 0.4572 mL 1.1430 mL
60 mM 0.0381 mL 0.1905 mL 0.3810 mL 0.9525 mL
80 mM 0.0286 mL 0.1429 mL 0.2858 mL 0.7144 mL
100 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5715 mL
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Z-VAD Related Classifications

Keywords:

Z-VAD162852-62-2CaspaseApoptosisAutophagyNecroptosiscompetitiveirreversibleradiationMDA-MB-231H460antiangiogenicInhibitorinhibitorinhibit

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