1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. SET2

SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases.

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

SET2 Chemical Structure

SET2 Chemical Structure

CAS No. : 2313525-20-9

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Description

SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases[1].

IC50 & Target[1]

TRPV2

0.46 μM (IC50)

In Vitro

SET2 (20 μM; 24 h) abrogates the migration of PC-3M cells expressing TRPV2[1].
SET2 (20 μM; 24 h) inhibits 2-APB-evoked current in HEK293T cells transiently co-transfected with TRPV2 and LPAR1[1].
SET2 (20 μM; 24 h) inhibits the increase of (0.1 μM; 3 min) LPA-induced cytoplasmic calcium and LPA-induced migration in PC-3M cells[1].

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

Cell Migration Assay [1]

Cell Line: PC-3M prostate cancer cells
Concentration: 0, 5 μM, 10 μM, and 20 μM
Incubation Time: 24 hr and 48 hr
Result: Inhibited cell migration of PC-3M cells, without inhibiting cell viability at 48 hours.
Molecular Weight

402.43

Formula

C17H21F3N4O2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CCSC1=NC(C(F)(F)F)=CC(N(CCC)C)=N1)NCC2=CC=CO2

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 : 100 mg/mL (248.49 mM; ultrasonic and warming and heat to 60°C; 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 2.4849 mL 12.4245 mL 24.8490 mL
5 mM 0.4970 mL 2.4849 mL 4.9698 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
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 2.4849 mL 12.4245 mL 24.8490 mL 62.1226 mL
5 mM 0.4970 mL 2.4849 mL 4.9698 mL 12.4245 mL
10 mM 0.2485 mL 1.2425 mL 2.4849 mL 6.2123 mL
15 mM 0.1657 mL 0.8283 mL 1.6566 mL 4.1415 mL
20 mM 0.1242 mL 0.6212 mL 1.2425 mL 3.1061 mL
25 mM 0.0994 mL 0.4970 mL 0.9940 mL 2.4849 mL
30 mM 0.0828 mL 0.4142 mL 0.8283 mL 2.0708 mL
40 mM 0.0621 mL 0.3106 mL 0.6212 mL 1.5531 mL
50 mM 0.0497 mL 0.2485 mL 0.4970 mL 1.2425 mL
60 mM 0.0414 mL 0.2071 mL 0.4142 mL 1.0354 mL
80 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7765 mL
100 mM 0.0248 mL 0.1242 mL 0.2485 mL 0.6212 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:
SET2
Cat. No.:
HY-132222
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