1. Metabolic Enzyme/Protease
    Apoptosis
    Autophagy
  2. Glutathione Peroxidase
    Apoptosis
    Autophagy
  3. NBDHEX

NBDHEX 

Cat. No.: HY-135318 Purity: 98.58%
Handling Instructions

NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.

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

NBDHEX Chemical Structure

NBDHEX Chemical Structure

CAS No. : 787634-60-0

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10 mM * 1 mL in DMSO USD 99 In-stock
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10 mg USD 150 In-stock
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Description

NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor[1][2].

IC50 & Target

Glutathione S-transferase P1-1 (GSTP1-1)[1];
Apoptosis[1];
Autophagy[1]

In Vitro

NBDHEX (0.05-20 μM; 48 hours; H69 and H69AR cells) is cytotoxic toward cell lung cancer H69 and H69AR cells[2].
NBDHEX (0-5 μM; 24 hours; H69AR cells) treatment results in a dose-dependent apoptosis in the H69AR cell line[2].
NBDHEX (3 μM; 1-12 hours; H69AR cells) treatment increases the phosphorylation of JNK/c-Jun in H69AR cells in a time-dependent fashion[2].
NBDHEX treatment shows a marked increase in phosphorylation of p38MAPK, and also increases GSSG content in a time-dependent manner in H69 cells[2].

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

Cell Viability Assay[2]

Cell Line: H69 and H69AR cells
Concentration: 0.05-20 μM
Incubation Time: 48 hours
Result: The dose-response profiles revealed a good cytotoxic activity both in sensitive H69 cell line (LC50 of 2.3 μM) and in its Adriamycin-resistant counterpart H69AR (LC50 of 4.5 μM).

Apoptosis Analysis[2]

Cell Line: H69AR cells
Concentration: 0 μM, 0.5 μM, 1 μM, 2 μM, 3 μM, 4 μM, 5 μM
Incubation Time: 24 hours
Result: Resulted in a dose-dependent apoptosis in the H69AR cell line.

Western Blot Analysis[2]

Cell Line: H69AR cells
Concentration: 3 μM
Incubation Time: 1 hour,3 hours, 6 hours, 12 hours
Result: Increased the phosphorylation of JNK/c-Jun in H69AR cells in a time-dependent fashion.
In Vivo

NBDHEX (0.8-80 mg/kg/day; oral administration; daily; for 15 days; SCID female mice) treatment results a statistically significant tumour inhibition (approximately 70%)[2].

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

Animal Model: SCID female mice (4-5 weeks) injected with Me501cells[3]
Dosage: 0.8 mg/kg/day, 8.0 mg/kg/day or 80 mg/kg/day
Administration: Oral administration; daily; for 15 days
Result: A statistically significant tumour inhibition (approximately 70%) was observed.
Molecular Weight

297.33

Formula

C₁₂H₁₅N₃O₄S

CAS No.

787634-60-0

SMILES

OCCCCCCSC1=CC=C([N+]([O-])=O)C2=NON=C21

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (420.41 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3633 mL 16.8163 mL 33.6327 mL
5 mM 0.6727 mL 3.3633 mL 6.7265 mL
10 mM 0.3363 mL 1.6816 mL 3.3633 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.00 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NBDHEXGlutathione PeroxidaseApoptosisAutophagyautophagyanticancercatalyticextrusioncytotoxicJNKc-JunGSSGp38MAPKInhibitorinhibitorinhibit

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