1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. Steppogenin

Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors.

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

Steppogenin Chemical Structure

Steppogenin Chemical Structure

CAS No. : 56486-94-3

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Based on 1 publication(s) in Google Scholar

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Description

Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. Steppogenin can be sued for the research of angiogenic diseases, such as those involving solid tumors[1].

IC50 & Target

IC50: 0.56 ± 0.043 μM (HIF-1α), 8.46 ± 1.08 μM (DLL4)[1]

In Vitro

Steppogenin (0-10 μM, 24 h) inhibit the transcriptional activity of HIF-1α under hypoxic conditions in HEK293T cells and VEGF-induced DLL4 expression in vascular endothelial cells (ECs) in a dose-dependent manner[1].
Steppogenin (0-3 μM, 6 h) suppresses the mRNA expression of HIF-1α target genes (VEGF, GLUT1, CXCR4, and CA9) under hypoxic conditions[1].
Steppogenin (0-3 μM, 16 h) suppresses HIF-1α protein levels, and inhibits protein levels of VEGF, CXCR4, and CA9[1].
Steppogenin (0-3 μM, 24 h) suppresses hypoxia-induced vascular EC proliferation and migration as well as VEGF-induced sprouting of EC spheroids[1].

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

RT-PCR[1]

Cell Line: A549 cells
Concentration: 0, 0.3, 1, 3 μM
Incubation Time: 6 h
Result: Suppressed the mRNA expression of HIF-1α target genes (VEGF, GLUT1, CXCR4, and CA9) under hypoxic conditions.

Western Blot Analysis[1]

Cell Line: HEK293T, A549, ARPE19 cells
Concentration: 0, 0.3, 1, 3 μM
Incubation Time: 16 h
Result: Significantly suppressed HIF-1α protein levels in a dose-dependent manner. reduced nuclear expression of HIF-1α under hypoxic conditions. Inhibited protein levels of VEGF, CXCR4, and CA9 compared with the levels detected in the vehicle control group. Suppresseed VEGF-induced DLL4 protein expression.
In Vivo

Steppogenin (2 mg/kg, IP, once) inhibits tumor growth and angiogenesis[1].
Steppogenin (2 mg/kg, IP, once) shows the highest distribution to the liver and spleen (25.5-fold and 9.74-fold AUC ratio, respectively) with significantly higher T1/2[1].
Pharmacokinetic Parameters of Steppogenin in male C57BL/6 J mice[1].

Cmax (ng/mL) Tmax (h) T1/2 (h) AUC8h (ng/mL∗h) AUC (ng/mL∗h) AUC ratio
Plasma 448 ± 113 0.25 0.49 ± 0.14 283 ± 98.9 284 ± 97.8 1
Tumor 635 ± 114 0.3 ± 0.1 1.87 ± 0.87 1078 ± 494 1252 ± 547 4.58
Liver 4319 ± 1063 0.25 1.72 ± 0.26 6733 ± 1300 6967 ± 1200 25.5
Lung 521 ± 181 0.25 0.36 ± 0.12 261 ± 96.1 280 ± 106 1.02
Heart 285 ± 15.2 0.25 0.2 107 ± 44.3 176.9 0.65
Kidney 1225 ± 463 0.25 0.33 ± 0.01 628 ± 234 624.7 ± 238 2.35
Spleen 6110 ± 2954 0.25 0.47 ± 0.01 2443 ± 1155 2663 ± 1289 9.74
Brain 309 ± 95.7 0.25 1.36 ± 0.46 191 ± 67 241 ± 75.4 0.88

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

Animal Model: C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)[1]
Dosage: 2 mg/kg
Administration: IP, once
Result: Significantly suppressed tumor growth.
Animal Model: C57BL/6 J mice (6-week-old, male, Lewis lung carcinoma (LLC) allograft tumor model)[1]
Dosage: 2 mg/kg
Administration: IP, once (Pharmacokinetic Analysis)
Result: Showed the highest distribution to the liver and spleen (25.5-fold and 9.74-fold AUC ratio, respectively) with significantly higher T1/2. may not be accumulated even in the highly distributed tissues after the repeated administration of steppogenin.
Molecular Weight

288.25

Formula

C15H12O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C[C@@H](C2=CC=C(O)C=C2O)OC3=CC(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 3 mg/mL (10.41 mM; Need ultrasonic and warming; 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 3.4692 mL 17.3461 mL 34.6921 mL
5 mM 0.6938 mL 3.4692 mL 6.9384 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 (protect from light). 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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Purity & Documentation

Purity: 99.49%

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 (protect from light). 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 3.4692 mL 17.3461 mL 34.6921 mL 86.7303 mL
5 mM 0.6938 mL 3.4692 mL 6.9384 mL 17.3461 mL
10 mM 0.3469 mL 1.7346 mL 3.4692 mL 8.6730 mL
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  • Do most proteins show cross-species activity?

    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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Steppogenin
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