Home > Products > Featured products

R-59949(R-59-949)

  Cat. No.:  DC23010   Featured
Chemical Structure
120166-69-0
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
A small molecule inhibitor of diacylglycerol kinase (DGK) with IC50 of 0.01-10 uM in isolated platelet membranes and in intact platelets.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 120166-69-0
Chemical Name: 3-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-2-sulfanylidene-1H-quinazolin-4-one
Synonyms: R59949;R 59949
SMILES: FC1C=CC(/C(/C2C=CC(F)=CC=2)=C2/CCN(CCN3C(=O)C4C(=CC=CC=4)NC3=S)CC/2)=CC=1
Formula: C28H25F2N3Os
M.Wt: 489.585
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC31074 Isopropyl myristate Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC74557 PREX-in1 PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.
DC74555 GYS32661 GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.
DC74539 L557-0155 L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.
DC74528 K284 K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.
DC74225 YB-537 YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).
DC74223 X-Neu5Ac X-Neu5Ac (sodium) is a substrate for chromogenic assay of neuraminidase activity in bacterial expression systems; with a Km of 0.89 mM for neuraminidase.
DC74218 UT-59 UT-59 is a specific inhibitor of cholesterol-sensing membrane protein Scap, binds to Scap's cholesterol-binding site, blocks SREBP activation and inhibits lipid synthesis.
DC74205 Tryptolinamide Tryptolinamide (TLAM) is a small-molecule compound that activates mitochondrial respiration in cybrids generated from patient-derived mitochondria and fibroblasts from patient-derived iPSCs, inhibits phosphofructokinase-1 (PFK1) with an ATP-uncompetitive
DC74203 TR-107 TR-107 (TR107) is a highly potent, selective and orally bioavailable small-molecule activator of the mitochondrial protease ClpP with EC50 of 140 nM, binds to purified ClpP with Kd value of 180 nM in surface plasmon resonance (SPR) measurement.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia