1. Metabolic Enzyme/Protease Apoptosis
  2. HIF/HIF Prolyl-Hydroxylase Apoptosis
  3. EL-102

EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer.

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

EL-102 Chemical Structure

EL-102 Chemical Structure

CAS No. : 1233948-61-2

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 237 In-stock
Solution
10 mM * 1 mL in DMSO USD 237 In-stock
Solid
1 mg USD 110 In-stock
5 mg USD 280 In-stock
10 mg USD 448 In-stock
50 mg USD 940 In-stock
100 mg USD 1410 In-stock
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Description

EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer[1].

IC50 & Target

IC50: 24 nM (CWR22), 21.7 nM (22Rv1), 40.3 nM (DU145), 37.0 nM (PC-3), 14.4 nM (DLKP), 16.3 nM (DLKPA)[1]

In Vitro

EL-102 (0-120 nM; 72 h) inhibits prostate cancer cells proliferation in vitro[1].
EL-102 (0-100 nM; 72 h) shows cytotoxicity to prostate cancer cell lines[1].
EL-102 (10-100 nM; 24-72 h) induces cellular apoptosis and affects cell cycle[1].
EL-102 (10-100 nM; 24-48 h) affects PARP cleavage in DU145 cells[1].
EL-102 (5 nM; 0-60 min) inhibits tubulin polymerisation activity[1].
EL-102 (0-100 nM; 1 hour) inhibits Hif1α protein expression[1].

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

Cell Proliferation Assay[1]

Cell Line: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines
Concentration: 0-120 nM
Incubation Time: 72 hours
Result: Inhibited proliferation of CWR22, 22Rv1, DU145, PC-3, DLKP and doxorubicin-selected variant DLKPA cells with IC50s of 24, 21.7, 40.3, 37.0, 14.4 and 16.3 nM, respectively.

Cell Cytotoxicity Assay[1]

Cell Line: CWR22, 22Rv1, DU145 and PC-3 cell lines
Concentration: 0-100 nM
Incubation Time: 72 hours
Result: Exibited cytotoxicity to prostate cancer cell lines, and showed no additive effect on the inhibition of cell viability with docetaxel.

Apoptosis Analysis[1]

Cell Line: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines
Concentration: 10 and 100 nM
Incubation Time: 24, 48 and 72 hours
Result: Induced cell apoptosis to inhibits cell viability with a dose of 100 nM.

Western Blot Analysis[1]

Cell Line: DU145 cell line
Concentration: 10 and 100 nM
Incubation Time: 24 and 48 hours
Result: Increased PARP cleavage in DU145 cells and showed a more dramatic effect with docetaxel adding.

Cell Cycle Analysis[1]

Cell Line: DU145 cell line
Concentration: 10 and 100 nM
Incubation Time: 24, 48 and 72 hours
Result: Increased loss of cells from G1 phase and accumulated cells in G2/M phase.

Western Blot Analysis[1]

Cell Line: Prostate cancer cells
Concentration: 10 , 50 and 100 nM
Incubation Time: 24 and 48 hours
Result: Modestly inhibited Hif1α expression at doses of 50 and 100 nM in normoxia.
In Vivo

EL-102 (12 and 15 mg/kg; p.o. 5-day on and 2-day off, from 13 to 37 days after tumour transplantation) potentiates effects of docetaxel in vivo[1].

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

Animal Model: Nude mice with CWR22 xenografts[1]
Dosage: 12 and 15 mg/kg
Administration: Oral gavage; 12 and 15 mg/kg 5-day on and 2-day off; from 13 to 37 days after tumour transplantation
Result: Showed no effect on tumor growth, but enhanced the effect of docetaxel on tumor .
Molecular Weight

384.47

Formula

C19H16N2O3S2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C1=CC=C(OC)C=C1)(NC2=CC(C3=CSC(C#N)=C3)=CC=C2C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 36 mg/mL (93.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6010 mL 13.0049 mL 26.0098 mL
5 mM 0.5202 mL 2.6010 mL 5.2020 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6010 mL 13.0049 mL 26.0098 mL 65.0246 mL
5 mM 0.5202 mL 2.6010 mL 5.2020 mL 13.0049 mL
10 mM 0.2601 mL 1.3005 mL 2.6010 mL 6.5025 mL
15 mM 0.1734 mL 0.8670 mL 1.7340 mL 4.3350 mL
20 mM 0.1300 mL 0.6502 mL 1.3005 mL 3.2512 mL
25 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6010 mL
30 mM 0.0867 mL 0.4335 mL 0.8670 mL 2.1675 mL
40 mM 0.0650 mL 0.3251 mL 0.6502 mL 1.6256 mL
50 mM 0.0520 mL 0.2601 mL 0.5202 mL 1.3005 mL
60 mM 0.0433 mL 0.2167 mL 0.4335 mL 1.0837 mL
80 mM 0.0325 mL 0.1626 mL 0.3251 mL 0.8128 mL
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Help & FAQs
  • 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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Product Name:
EL-102
Cat. No.:
HY-16187
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