1. Anti-infection Metabolic Enzyme/Protease
  2. Antibiotic Phosphatase Fungal
  3. Roridin E

Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies.

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Roridin E

Roridin E Chemical Structure

CAS No. : 16891-85-3

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Description

Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies[1][2][3].

Cellular Effect
Cell Line Type Value Description References
A549 IC50
< 9.7 μM
Compound: Roridin E
Cytotoxicity against human A549 cells after 72 hrs
Cytotoxicity against human A549 cells after 72 hrs
[PMID: 21907583]
BT-549 IC50
uM μM
Compound: 4
Cytotoxicity against human BT549 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human BT549 cells assessed as growth inhibition after 72 hrs by SRB assay
[PMID: 30457333]
HCC70 IC50
uM μM
Compound: 4
Cytotoxicity against human HCC70 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human HCC70 cells assessed as growth inhibition after 72 hrs by SRB assay
[PMID: 30457333]
HL-60 IC50
0.3 ng/mL
Compound: 2
Cytotoxicity against human HL60 cells after 72 hrs by WST8 assay
Cytotoxicity against human HL60 cells after 72 hrs by WST8 assay
[PMID: 11277768]
K562 IC50
0.54 μM
Compound: 11
Cytotoxicity against human K562 cells by disk diffusion soft agar colony formation assay
Cytotoxicity against human K562 cells by disk diffusion soft agar colony formation assay
[PMID: 31117520]
KB EC50
0.5 ng/mL
Compound: 4
Cytotoxicity against human KB cells
Cytotoxicity against human KB cells
[PMID: 10075777]
L1210 IC50
0.2 ng/mL
Compound: 2
Cytotoxicity against mouse L1210 cells after 72 hrs by WST8 assay
Cytotoxicity against mouse L1210 cells after 72 hrs by WST8 assay
[PMID: 11277768]
MDA-MB-231 IC50
uM μM
Compound: 4
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by SRB assay
[PMID: 30457333]
MDA-MB-468 IC50
uM μM
Compound: 4
Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 72 hrs by SRB assay
Cytotoxicity against human MDA-MB-468 cells assessed as growth inhibition after 72 hrs by SRB assay
[PMID: 30457333]
SW 1116 IC50
0.039 μM
Compound: 11
Cytotoxicity against human SW1116 cells by disk diffusion soft agar colony formation assay
Cytotoxicity against human SW1116 cells by disk diffusion soft agar colony formation assay
[PMID: 31117520]
Vero EC50
0.4 ng/mL
Compound: 4
Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
[PMID: 10075777]
In Vivo

Roridin E (2 mg/kg; s.c.; single dose) produces a significant increase in liver glucose-6-phosphatase activity and kidney glutathione levels, with no significant changes in other measured serum, liver, or kidney biochemical parameters in male Sprague-Dawley rats[1].
Roridin E (2 mg/kg; i.p.; single dose) induces significant hepatotoxicity in male albino mice, as evidenced by increased liver oxidative stress markers and altered serum liver function parameters[2].

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

Animal Model: Sprague-Dawley (male, 150-170 g)[1]
Dosage: 2 mg/kg
Administration: s.c.; single dose
Result: Showed no significant changes in levels of TBARS, total lipids, glucose, glutathione, creatinine, zinc, or calcium in serum compared to controls.
Increased liver glucose-6-phosphatase activity to 10.6 nmol/min/mg proteins, with no significant changes in TBARS, total lipid, glutathione, 5-nucleotidase, or superoxide dismutase levels in liver compared to controls.
Increased kidney glutathione level to 6.76 μg/mg proteins, with no significant changes in TBARS, total lipid, 5-nucleotidase, glucose-6-phosphatase, or superoxide dismutase levels in kidney compared to controls.
Animal Model: albino mice (male, 6 weeks old, 20-25 g)[2]
Dosage: 2 mg/kg
Administration: i.p.; single dose
Result: Increased liver tissue TBARs to 2.3 mmol/mL.
Increased liver tissue SOD to 1.9 ng/mL.
Increased liver tissue GSH to 2.9 mmol/mL.
Decreased blood serum total protein to 4.4 g/dl.
Increased blood serum total lipids to 5.8 mg/mL.
Increased blood serum GGT to 32.1 u/mL.
Increased blood serum alkaline phosphatase to 116 u/L.
Increased blood serum 5'-nucleotidase to 1.8 u/mL.
Molecular Weight

514.61

Formula

C29H38O8

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@]3(CO3)[C@@]4([H])C[C@@]1([H])OC(/C=C\C=C\[C@@]([C@H](O)C)([H])OCC/C(C)=C/C(OC[C@]25[C@](C=C(C)CC5)([H])O4)=O)=O

Structure Classification
Initial Source

Myrothecium verrucaria

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 99.82%

References
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Roridin E
Cat. No.:
HY-125539
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