Structure of Didox
CAS No.: 69839-83-4
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Didox can prevent LPS-induced NF-KB activation and translocation of NF-kappa beta p65 subunits.
Synonyms: NSC-324360
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Batch number can be found on the product's label following the word 'Batch'.
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Batch number can be found on the product's label following the word 'Batch'.
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CAS No. : | 69839-83-4 |
Formula : | C7H7NO4 |
M.W : | 169.13 |
SMILES Code : | O=C(NO)C1=CC=C(O)C(O)=C1 |
Synonyms : |
NSC-324360
|
MDL No. : | MFCD01667810 |
InChI Key : | QJMCKEPOKRERLN-UHFFFAOYSA-N |
Pubchem ID : | 3045 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
Target |
|
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
ARPE-19 epithelial cells | 182 ± 23 µM (EC50) | 14 days | To evaluate the anti-HCMV activity of Didox when used alone, the results showed an EC50 of 182 ± 23 µM in ARPE-19 cells. | PMC3843955 |
MRC-5 fibroblasts | 82 ± 32 µM (EC50) | 14 days | To evaluate the anti-HCMV activity of Didox when used alone, the results showed an EC50 of 82 ± 32 µM in MRC-5 cells. | PMC3843955 |
T-cells (B10.D2 and C57BL6 mice) | 25 μM - 100 μM | 24 - 48 hours | Didox significantly inhibited the secretion of cytokines IL-6, IFN-γ, TNF-α, IL-2, IL-13, IL-10 and IL-4. | PMC2933664 |
Mouse embryonic fibroblast (MEF) | 25 μM - 100 μM | 24 - 96 hours | Didox significantly inhibited T-cell proliferation, with 25μM concentration reducing proliferation by approximately 90% at 96 hours post stimulation, and 50μM concentration completely blocking proliferation. | PMC2933664 |
MDA-MB-468 | 30-600 μM | 24 hours | Didox downregulates cyclin D1, cyclin A2, and cyclin E2, along with NF-κB signaling proteins p100, p105, and RelB, and increases Rb and pRb S807 expression. | PMC10930692 |
MCF7 | 30-600 μM | 24 hours | Didox downregulates an element of the cell cycle checkpoint, cyclin D1, accompanied by a reduction in NF-κB activity and induces cell cycle arrest at G1. | PMC10930692 |
Mouse primary cardiomyocytes | 1 μM | 24 hours | To investigate the effect of DOX on RRM2 expression, results showed decreased RRM2 mRNA and protein levels | PMC8869767 |
RAW264.7 macrophages | 50 μM | 24 hours | To evaluate the effects of Didox on LPS-induced inflammation and oxidative stress. Results showed that Didox significantly inhibited the mRNA expression of iNOS, IL-6, TNF-α, and COX-2, and reduced the secretion of NO, IL-6, and IL-10. | PMC4408267 |
HuH7 cells | 1, 10, 25, 50, 100, 200 and 500 µM | 24, 48 and 72 hours | Didox showed similar sensitivity in HuH7 cells with IC50 of 329.31 ± 31.55 µM at 48 h and 122.92 ± 13.21 µM at 72 h. | PMC6789654 |
HA22T/VGH cells | 1, 10, 25, 50, 100, 200 and 500 µM | 24, 48 and 72 hours | Didox reduced cell viability in a dose- and time-dependent manner with IC50 of 283.36 ± 18.82 µM at 48 h and 132.98 ± 7.97 µM at 72 h. | PMC6789654 |
SH-SY5Y | 10 µM | 3 hours | To evaluate the activation effect of Didox on HIF1 ODD-luc and Neh2-luc reporters. Results showed that Didox activated HIF1 ODD-luc reporter at concentrations above 100 µM but had no effect on Neh2-luc reporter. | PMC5201116 |
MRC-5 fibroblasts | 103 ± 19 µM (EC50) | 5 days | To evaluate the anti-HCMV activity of Didox when used alone, the results showed an EC50 of 103 ± 19 µM in MRC-5 cells. | PMC3843955 |
Peritoneal mast cells | 100 μM | 6 hours | Didox significantly suppressed IL-33-induced IL-6 production | PMC5593780 |
Bone marrow derived mast cells (BMMC) | 100 μM | 6 hours | Didox significantly suppressed IL-33-induced production of IL-6, IL-13, TNF, and MIP-1α | PMC5593780 |
Peritoneal mast cells | 100 µM | 6 hours | Didox suppressed IgE-mediated IL-6 and IL-13 secretion but had no significant effect on MCP-1. | PMC5733711 |
Mouse bone marrow-derived mast cells (BMMC) | 100 µM | 6 hours | Didox suppressed IgE-stimulated degranulation and cytokine production, including IL-6, IL-13, TNF, and MIP-1a. | PMC5733711 |
HT-29 | 501.6 ± 53 μM (IC50) | 72 hours | To evaluate the cytotoxic effect of Didox on HT-29 cells, results showed an IC50 of 501.6 ± 53 μM for Didox alone. | PMC5107943 |
HCT 116 | 105 ± 1.5 μM (IC50) | 72 hours | To evaluate the cytotoxic effect of Didox on HCT 116 cells, results showed an IC50 of 105 ± 1.5 μM for Didox alone. | PMC5107943 |
MCF-7 cells | 9.506 ± 0.08 μg/ml (IC50) | 72 hours | Evaluate the effect of Didox on Herceptin cytotoxicity, results showed that Didox combined with Herceptin significantly reduced the IC50 value, indicating synergistic effect | PMC4496837 |
T47D cells | 82.975 ± 5.95 μg/ml (IC50) | 72 hours | Evaluate the effect of Didox on Herceptin cytotoxicity, results showed that Didox combined with Herceptin significantly reduced the IC50 value, indicating synergistic effect | PMC4496837 |
H9C2 cells | 60 μM | To investigate the effect of RRM2 on cell proliferation, results showed RRM2 overexpression reduced adverse effects of DOX on proliferation | PMC8869767 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
C57/B6 mice | DOX-induced cardiomyopathy model | Intraperitoneal injection | 15 mg/kg | 5 days | To investigate the role of RRM2 in DOX-induced cardiomyopathy, results showed RRM2 overexpression alleviated myocardial injury | PMC8869767 |
Mice (C57BL6 and B10.D2) | Mixed lymphocyte reaction (MLR) model | In vitro culture | 25 μM - 100 μM | Single treatment, lasting 6 days | Didox significantly inhibited T-cell proliferation and cytokine secretion in MLR, with 100μM dose inhibiting IFN-γ and IL-2 production to levels comparable to normal controls. | PMC2933664 |
Mice | LPS-induced neuroinflammation model | Intraperitoneal injection | 250 mg/kg | Starting 24 h post-LPS injection and continued for 6 days | Didox treatment reversed AIS disruption and accelerated AIS recovery. | PMC5465457 |
C57BL/6J mice | IgE-mediated passive systemic anaphylaxis model | Intraperitoneal (IP) injection | 350 mg/kg | Single dose, 6 hours before anaphylaxis induction | Didox significantly attenuated the temperature drop in IgE-mediated passive systemic anaphylaxis. | PMC5733711 |
Nude mice | MCF7 PR breast cancer model | Intraperitoneal injection | 425 mg/kg/day | Once daily for 9 days | Didox alone or in combination with palbociclib significantly inhibited the growth of ER+ palbociclib-resistant tumors. | PMC10930692 |
Tags: Didox | NSC-324360 | NSC324360 | NSC 324360 | DNA/RNA Synthesis | ribonucleotide reductase inhibitor | DNA synthesis | 69839-83-4
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