R59949

Modify Date: 2024-01-06 12:38:11

R59949 Structure
R59949 structure
Common Name R59949
CAS Number 120166-69-0 Molecular Weight 489.57900
Density 1.36g/cm3 Boiling Point 637.1ºC at 760mmHg
Molecular Formula C28H25F2N3OS Melting Point N/A
MSDS Chinese USA Flash Point 339.1ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of R59949


R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol[1][2][3].

 Names

Name 3-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-2-sulfanylidene-1H-quinazolin-4-one
Synonym More Synonyms

 R59949 Biological Activity

Description R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol[1][2][3].
Related Catalog
In Vitro In the presence of R59949, vasopressin- as well as collagen-induced release reaction and aggregation was strongly increased, independently of the formation of arachidonate metabolites[1]. In THP‐1 monocytes, R59949 attenuates CCL2‐evoked Ca2+ signalling with a half‐maximal concentration of 8.6 μM[2]. R59949 inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells[4].
References

[1]. de Chaffoy de Courcelles D, et al. The role of endogenously formed diacylglycerol in the propagation and termination of platelet activation. A biochemical and functional analysis using the novel diacylglycerol kinase inhibitor, R 59 949. J Biol Chem. 1989;264(6):3274-3285.

[2]. Day P, et al. Inhibitors of DAG metabolism suppress CCR2 signalling in human monocytes. Br J Pharmacol. 2019;176(15):2736-2749.

[3]. Meinhardt G, et al. Effect of novel modulators of protein kinase C activity upon chemotherapy-induced differentiation and apoptosis in myeloid leukemic cells. Anticancer Drugs. 2002;13(7):725-733.

[4]. Shimomura T, et al. R59949, a diacylglycerol kinase inhibitor, inhibits inducible nitric oxide production through decreasing transplasmalemmal L-arginine uptake in vascular smooth muscle cells. Naunyn Schmiedebergs Arch Pharmacol. 2017;390(2):207-214.

 Chemical & Physical Properties

Density 1.36g/cm3
Boiling Point 637.1ºC at 760mmHg
Molecular Formula C28H25F2N3OS
Molecular Weight 489.57900
Flash Point 339.1ºC
Exact Mass 489.16900
PSA 73.12000
LogP 5.87310
Vapour Pressure 3.94E-16mmHg at 25°C
Index of Refraction 1.688
Storage condition -20°C

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H315-H319-H335
Precautionary Statements P261-P305 + P351 + P338
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes Xi
Risk Phrases R36/37/38
Safety Phrases S26-S36
RIDADR NONH for all modes of transport

 Articles33

More Articles
Diacylglycerol kinase α promotes 3D cancer cell growth and limits drug sensitivity through functional interaction with Src.

Oncotarget 5(20) , 9710-26, (2014)

Diacylglycerol kinase (DGK)α converts diacylglycerol to phosphatidic acid. This lipid kinase sustains survival, migration and invasion of tumor cells, with no effect over untransformed cells, suggesti...

Insulin action on polyunsaturated phosphatidic acid formation in rat brain: an "in vitro" model with synaptic endings from cerebral cortex and hippocampus.

Neurochem. Res. 34(7) , 1236-48, (2009)

The highly efficient formation of phosphatidic acid from exogenous 1-stearoyl-2-arachidonoyl-sn-glycerol (SAG) in rat brain synaptic nerve endings (synaptosomes) from cerebral cortex and hippocampus i...

Effect of novel modulators of protein kinase C activity upon chemotherapy-induced differentiation and apoptosis in myeloid leukemic cells.

Anticancer Drugs 13(7) , 725-33, (2002)

Modulation of protein kinase C (PKC) activity has been demonstrated to either prevent or enhance drug-induced apoptosis in various tissue types. We tested four novel modulators of PKC activity in comp...

 Synonyms

MFCD00069258
Diacylglycerol Kinase Inhibitor II
Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: R-59949
  • Price: $Inquiry/25mg $Inquiry/100mg $Inquiry/500mg
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao


Get all suppliers and price by the below link:

R59949 suppliers


Price: ¥2700/5 mg

Reference only. check more R59949 price

Hot Compounds More...
Dichloromethane
CAS#:75-09-2
Polyacrylic acid
CAS#:9003-01-4
sodium carbonate
CAS#:497-19-8
Silicon dioxide
CAS#:7631-86-9
Triethanolamine
CAS#:102-71-6
Demeton
CAS#:126-75-0
Water
CAS#:7732-18-5
4-(4-Piperidinyl)morpholine dihydrochloride
CAS#:53617-35-9
Diclofenac sodium
CAS#:15307-79-6
Budesonide
CAS#:51372-29-3