Date published: 2026-2-22

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PAR-4 Activators

PAR-4 activators constitute a distinct category of chemical compounds that interact with the Proteinase-Activated Receptor 4 (PAR-4) protein, a member of the PAR family of G-protein-coupled receptors (GPCRs). PAR-4 is primarily expressed in various tissues throughout the human body and is known to play a pivotal role in cellular signaling and physiological responses. When activated by specific compounds, PAR-4 undergoes conformational changes that lead to the activation of intracellular signaling pathways, such as the activation of G-proteins and downstream effector molecules. These molecular events can trigger a cascade of cellular responses, influencing various physiological processes.

The activation of PAR-4 receptors can have diverse effects on different cell types and tissues, as PAR-4 is widely distributed throughout the body. These activators may influence processes ranging from platelet activation and coagulation to immune responses and pain perception. Understanding the chemical properties and mechanisms underlying PAR-4 activation is crucial for elucidating the intricate signaling pathways that govern cellular responses mediated by this receptor. Research in this field can provide insights into the broader landscape of GPCR signaling, shedding light on how specific compounds can modulate PAR-4 function and contributing to a deeper understanding of cellular physiology and pathophysiology.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Doxorubicin

23214-92-8sc-280681
sc-280681A
1 mg
5 mg
$176.00
$426.00
43
(3)

Doxorubicin functions as a topoisomerase II inhibitor and induces DNA damage, which has been shown to upregulate PAR-4 expression levels.

Etoposide (VP-16)

33419-42-0sc-3512B
sc-3512
sc-3512A
10 mg
100 mg
500 mg
$51.00
$231.00
$523.00
63
(1)

Etoposide is a semisynthetic derivative of podophyllotoxin that acts as a topoisomerase II inhibitor. By inhibiting topoisomerase II and inducing DNA damage, etoposide treatment has been found to increase PAR-4 protein levels in various cancer cell lines.

Cisplatin

15663-27-1sc-200896
sc-200896A
100 mg
500 mg
$138.00
$380.00
101
(4)

Cisplatin is a platinum-based chemotherapeutic agent known to induce apoptotic cell death. Studies demonstrate that cisplatin treatment results in enhanced PAR-4 expression, contributing to its proapoptotic effects in glioma and testicular cancer cells.

Hydroxyurea

127-07-1sc-29061
sc-29061A
5 g
25 g
$78.00
$260.00
18
(1)

As a ribonucleotide reductase inhibitor, hydroxyurea causes DNA damage by depleting the deoxynucleotide triphosphate pool. The induced DNA damage has been linked to transcriptional upregulation of PAR-4 in cancer models.

Camptothecin

7689-03-4sc-200871
sc-200871A
sc-200871B
50 mg
250 mg
100 mg
$58.00
$186.00
$94.00
21
(2)

Camptothecin is a plant alkaloid featuring a lactone ring that interferes with topoisomerase I function and DNA repair. Studies show camptothecin treatment boosts PAR-4 promoter activity and protein levels in prostate and ovarian cancer cells.

Dexamethasone

50-02-2sc-29059
sc-29059B
sc-29059A
100 mg
1 g
5 g
$91.00
$139.00
$374.00
36
(1)

As a synthetic glucocorticoid, dexamethasone triggers apoptosis in lymphoid tissues. Research links this effect with dexamethasone's capacity to transactivate the PAR-4 promoter and induce PAR-4 mRNA transcription in T cells.

Triptolide

38748-32-2sc-200122
sc-200122A
1 mg
5 mg
$90.00
$204.00
13
(1)

isolated from the herb Tripterygium wilfordii, triptolide causes DNA damage and mitochondrial dysfunction. It activates PAR-4 expression dose-dependently in glioma cells, suggesting an antitumor mechanism.

Cucurbitacin I

2222-07-3sc-203010
1 mg
$250.00
9
(1)

A tetracyclic triterpenoid isolated from Cucurbitaceae plants, cucurbitacin I demonstrates antitumor properties associated with PAR-4 induction in renal carcinoma and melanoma cell lines.

Genistein

446-72-0sc-3515
sc-3515A
sc-3515B
sc-3515C
sc-3515D
sc-3515E
sc-3515F
100 mg
500 mg
1 g
5 g
10 g
25 g
100 g
$45.00
$164.00
$200.00
$402.00
$575.00
$981.00
$2031.00
46
(1)

Genistein is a isoflavone found in soy. Studies associate this compound's estrogen-modulating activity with transcriptional induction of PAR-4 in ovarian and breast cancer models.