Giripladib - CAS 865200-20-0
Catalog number: 865200-20-0
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C41H36ClF3N2O4S
Molecular Weight:
745.25
COA:
Inquire
Targets:
Phospholipase
Description:
Giripladib is a Phospholipase A2 inhibitor. Treatment with Giripladib attenuated radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. Giripladib in combination with irradiation significantly reduced migration and proliferation in endothelial cells and induced cell death and attenuated invasion by tumor cells.
Publictions citing BOC Sciences Products
  • >> More
Purity:
98%
Appearance:
Powder
Synonyms:
4-[3-[5-Chloro-1-(diphenylmethyl)-2-[2-[[[[2-(trifluoromethyl)phenyl]methyl]sulfonyl]amino]ethyl]-1H-indol-3-yl]propyl]benzoic Acid; 4-(3-[5-Chloro-1-(diphenylmethyl)-2-[2-(((2-(trifluoromethyl)benzyl)sulfonyl)amino)ethyl]-1H-indole-3-yl]propyl)benzoic Acid; PLA 695
Solubility:
Soluble in DMSO
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
antitumor
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
Density:
1.29
InChIKey:
NHHBNHIPCSPSHQ-UHFFFAOYSA-N
InChI:
1S/C41H36ClF3N2O4S/c42-33-22-23-37-35(26-33)34(16-9-10-28-18-20-31(21-19-28)40(48)49)38(47(37)39(29-11-3-1-4-12-29)30-13-5-2-6-14-30)24-25-46-52(50,51)27-32-15-7-8-17-36(32)41(43,44)45/h1-8,11-15,17-23,26,39,46H,9-10,16,24-25,27H2,(H,48,49)
Canonical SMILES:
c1ccc(cc1)C(c2ccccc2)n3c4ccc(cc4c(c3CCNS(=O)(=O)Cc5ccccc5C(F)(F)F)CCCc6ccc(cc6)C(=O)O)Cl
Current Developer:
Originator Wyeth
1.Cytosolic phospholipaseA2 inhibition with PLA-695 radiosensitizes tumors in lung cancer animal models.
Thotala D1, Craft JM, Ferraro DJ, Kotipatruni RP, Bhave SR, Jaboin JJ, Hallahan DE. PLoS One. 2013 Jul 19;8(7):e69688. doi: 10.1371/journal.pone.0069688. Print 2013.
Lung cancer remains the leading cause of cancer deaths in the United States and the rest of the world. The advent of molecularly directed therapies holds promise for improvement in therapeutic efficacy. Cytosolic phospholipase A2 (cPLA2) is associated with tumor progression and radioresistance in mouse tumor models. Utilizing the cPLA2 specific inhibitor PLA-695, we determined if cPLA2 inhibition radiosensitizes non small cell lung cancer (NSCLC) cells and tumors. Treatment with PLA-695 attenuated radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells. NSCLC cells (LLC and A549) co-cultured with endothelial cells (bEND3 and HUVEC) and pre-treated with PLA-695 showed radiosensitization. PLA-695 in combination with irradiation (IR) significantly reduced migration and proliferation in endothelial cells (HUVEC & bEND3) and induced cell death and attenuated invasion by tumor cells (LLC &A549). In a heterotopic tumor model, the combination of PLA-695 and radiation delayed growth in both LLC and A549 tumors.
2.Platelet Lipidomic Profiling: Novel Insight into Cytosolic Phospholipase A2α Activity and Its Role in Human Platelet Activation.
Duvernay MT1, Matafonov A2, Lindsley CW3, Hamm HE1. Biochemistry. 2015 Sep 15;54(36):5578-88. doi: 10.1021/acs.biochem.5b00549. Epub 2015 Sep 1.
With a newer, more selective and efficacious cytosolic phospholipase A2α (cPLA2α) inhibitor available, we revisited the role of cPLA2α activity in platelet activation and discovered that a component of platelet signaling, even larger than previously appreciated, relies on this enzyme. In a whole blood shear-based flow chamber assay, giripladib, a cPLA2α inhibitor, reduced platelet adhesion and accumulation on collagen. Moreover, giripladib differentially affected P-selectin expression and GPIIbIIIa activation depending on the agonist employed. While protease-activated receptor 1 (PAR1)-mediated platelet activation was unaffected by giripladib, the levels of PAR4- and GPVI-mediated platelet activation were significantly reduced. Meanwhile, the thromboxane A2 receptor antagonist SQ29548 had no effect on PAR-, GPVI-, or puriniergic receptor-mediated platelet activation, suggesting that another eicosanoid produced downstream of arachidonic acid liberation by cPLA2α was responsible for this large component of PAR4- and GPVI-mediated platelet activation.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Phospholipase Products


CAS 112648-68-7 U-73122

U-73122
(CAS: 112648-68-7)

U-73122 is a phospholipase C inhibitor originated by Pharmacia Corporation and IC 50 value is 1.0-2.1 μM in neutrophils and human platelets. U-73122 can be used...

FIPI hydrochloride
(CAS: 1781834-93-2)

FIPI hydrochloride is an inhibitor of phospholipase D (PLD) (IC50 values of 20-25 nM for both PLD1 and PLD2), which is an enzyme catalyzing the hydrolysis of ph...

CAS 172732-68-2 Varespladib

Varespladib
(CAS: 172732-68-2)

Varespladib is a potent and selective inhibitor of secretory phospholipase A2 (sPLA2). The compound Varespladib inhibits both human and mouse sPLA2 group IIA, V...

CAS 83373-60-8 D609

D609
(CAS: 83373-60-8)

D609 is a selective competitive phosphatidyl choline-specific phospholipase C (PC-PLC) inhibitor and is antiviral and antitumor agent. It suppresses LPS- and IF...

CAS 1845753-81-2 AZD2716

AZD2716
(CAS: 1845753-81-2)

AZD2716 is a potent sPLA2 inhibitor (IC50 = 10, 40, and 400 nM for sPLA2-IIa, -V, and -X, respectively). When incubated with HepG2 cells, AZD2716 effectively in...

CAS 356057-34-6 Darapladib

Darapladib
(CAS: 356057-34-6)

Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM.

CAS 479422-22-5 CDIBA

CDIBA
(CAS: 479422-22-5)

CDIBA is a potent and selective cytosolic phospholipase A2 (cPLA2) inhibitor.

CAS 1233706-88-1 CAY10650

CAY10650
(CAS: 1233706-88-1)

Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a...

CAS 899713-86-1 ML348

ML348
(CAS: 899713-86-1)

ML348, also known as CID 3238952 or SID 160654487, is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM). It is 14-fold selective...

BMS-229724
(CAS: 221914-85-8)

BMS-229724 is a selective tight-binding inhibitor of cytosolic phospholipase A2 (cPLA2) in that it did not inhibit secreted phospholipase A2 in vitro, nor phosp...

CAS 69-05-6 Quinacrine hydrochloride

Quinacrine hydrochloride
(CAS: 69-05-6)

Quinacrine dihydrochloride is the dihydrochloride salt of the 9-aminoacridine derivative quinacrine with potential antineoplastic and antiparasitic activities. ...

CAS 1404456-53-6 GSK2830371

GSK2830371
(CAS: 1404456-53-6)

GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.

LY-178002
(CAS: 107889-32-7)

LY-178002 is a phospholipase A2 inhibitor. It also inhibits leukotriene B4 production.

CAS 865200-20-0 Giripladib

Giripladib
(CAS: 865200-20-0)

Giripladib is a Phospholipase A2 inhibitor. Treatment with Giripladib attenuated radiation induced increases of phospho-ERK and phospho-Akt in endothelial cells...

CAS 1096687-52-3 SPK-601

SPK-601
(CAS: 1096687-52-3)

SPK-601 is a potent phosphatidylcholine-specific phospholipase C (PC-PLC) inhibitor,a useful antimicrobial agent.

CAS 1312782-34-5 AA26-9

AA26-9
(CAS: 1312782-34-5)

AA26-9, synthesized based on a piperazine scaffold, is a potent and broad spectrum serine hydrolase inhibitor.

Chemical Structure

CAS 865200-20-0 Giripladib

Quick Inquiry

Verification code

Featured Items