Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName NSC23766 Cat No CEI-0847 Description NSC 23766 is an inhibitor of RacGTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM; does not inhibit the closely related targetsCdc42 or RhoA. CAS No 1177865-17-6 Molecular Weight 530.96 Storage 2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO. Targets Rac GTPase IC50 50 μM Molecular Formula C24H35N7.3HCl Chemical Name N6-[2-[[4-(Diethylamino)-1-methylbu-tyl]amino]-6-methyl-4-pyrimidinyl]-2-methyl-4,6-qu-inolinediamine trihydrochloride Solubility DMSO 106 mg/mL; Water 106 mg/mL; Ethanol 5 mg/mL In vitro NSC23766 is identified to fit into a surface groove of Rac1 known to be critical for GEF specification. NSC23766 effectively inhibits Rac1 binding and activation by the Rac-specific GEF Trio or Tiam1 in a dose-dependent manner without interfering with the closely related Cdc42 or RhoA binding or activation by their respective GEFs or with Rac1 interaction with BcrGAP or effector PAK1. NSC 23766 is active in regulating Rac GTPase functions on cytoskeleton and many cell functions including cell cycle, cell growth, adhesion, migration and gene transcription. NSC 23766 (50 μM) potently blocks serum or platelet-derived growth factor-induced Rac1 activation and lamellipodia formation without affecting the activity of endogenous Cdc42 or RhoA in NIH 3T3 cells. NSC 23766 reduces Trio or Tiam1 but not Vav, Lbc, Intersectin, or a constitutively active Rac1 mutant-stimulated NIH 3T3 cells growth and suppresses Trio, Tiam1, or Ras-induced cell transformation. NSC23766 dose-dependently inhibits PC-3 cells proliferation and anchorage-independent growth. 25 μM NSC23766 inhibits the PC-3 cell invasion through Matrigel by 85%. 50 μM NSC 23766 inhibits thrombin-induced activation of Rac1 an d Rac2 in human platelets, as well as platelet aggregation.NSC23766 prevents Aβ40 and Aβ42 production in swAPP-HEK293cells without affecting Notch and sAPPα. NSC23766 prevents γ-secretase activity in cell, but not act as a direct γ-secretase inhibitor. NSC23766 dose-dependently reduces levels of secreted and intracellular Aβ40 with IC50 of 48.94 μM. 50 μM NSC 23766 inhibits release of Aβ42 by 57.97%.NSC23766 regulates endothelial nitric oxide synthase expression and endothelial function. 100 μM NSC23766 represses the eNOS promoter activity by 60% in bovine aortic ECs and by 30% to 35% in bEND.3 cells. Inhibition of Rac1 with NSC23766 destabilizes eNOS mRNA and shortens its half-life to 17 hours. NSC23766 dose-dependently attenuates ACh-induced relaxation of wild-type mice aortic rings.NSC23766 inhibits cell growth and induces apoptosis. NSC23766 decreases MDA-MB-468 and MDA-MB-231 cells viability in a dose-dependent manner with IC50 of ~10 μM, which is not correlated with the status of estrogen receptor (ER), progesterone receptor (PR), Her2, and p53 mutation. NSC23766 has little effect on the survival of the MCF12A normal mammary epithelial cells. After 24 hours expose to NSC 23766, MDA-MB-231 cells showes an increase from 41% to 65% in G1 phase and a concomitant decrease in S and G2-M phases. 100 μM NSC23766 induces a six-fold increase of apoptotic MDA-MB-468. The inhibition of NSC23766 on cell cycle arrest or apoptosis in breast cancer cells is mediated by downregulation of cyclin D1, survivin, and X-linked inhibitor of protein apoptosis. In vivo NSC23766 induces mobilization of hematopoietic stem cells/progenitors. Intraperitoneal administration of NSC23766 (2.5 mg/kg) into the ‘‘poorly mobilizing ’’ C57Bl/6 mouse strain leads to a two-fold increase in circulating hematopoietic stem cells/progenitors 6 hr after injection.NSC23766 alleviates lipopolysaccharide-induced acute pulmonary injury in mice. Treatment with NSC23766 at 1 or 3mg/kg not only reduces the inflammatory cells infiltration and MPO activities, but also inhibits pro-inflammatory mediators, tumor necrosis factor-α and interleukin-1β, mRNA expression. NSC23766 also reduces Evans Blue and albumin accumulation in LPS-challenged lungs. category Inhibitors(c1514) cas_num 1177865-17-6 Basic Info-
Product Name:
NSC 23766 (hydrochloride)
Other Name:NSC 23766 (hydrochloride);NSC 23766 (trihydrochloride);NSC23766 trihydrochloride;NSC-23766 trihydrochloride;N6-[2-(4-Diethylamino-1-methyl-butylamino)-6-methyl-pyrimidin-4-yl]-2-methyl-quinoline-4,6-diamine trihydrochloride;NSC-23766 HCl;NSC 23766, >=98%;Rac1 Inhibitor
CAS No.:1177865-17-6
Molecular Formula:C24H35N7.3HCl
InChIKeys:CPUHORIUXPQCHW-UHFFFAOYSA-N
Molecular Weight:530.967
Exact Mass:529.225
Categories:
Characteristics-
PSA:
92
XLogP3:5.61700
Appearance:white to beige
Water Solubility:H2O: soluble10mg/mL, clear
Storage Conditions:-20°C
Hazard IdentificationClassification of the substance or mixture
Skin irritation, Category 2
Eye irritation, Category 2
Specific target organ toxicity â single exposure, Category 3
GHS label elements, including precautionary statements
Pictogram(s) 
Signal word Warning
Hazard statement(s) H315 Causes skin irritation
H319 Causes serious eye irritation
H335 May cause respiratory irritation
Precautionary statement(s) Prevention P264 Wash ... thoroughly after handling.
P280 Wear protective gloves/protective clothing/eye protection/face protection/hearing protection/...
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P271 Use only outdoors or in a well-ventilated area.
Response P302+P352 IF ON SKIN: Wash with plenty of water/...
P321 Specific treatment (see ... on this label).
P332+P317 If skin irritation occurs: Get medical help.
P362+P364 Take off contaminated clothing and wash it before reuse.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P304+P340 IF INHALED: Remove person to fresh air and keep comfortable for breathing.
P319 Get medical help if you feel unwell.
Storage P403+P233 Store in a well-ventilated place. Keep container tightly closed.
P405 Store locked up.
Disposal P501 Dispose of contents/container to an appropriate treatment and disposal facility in accordance with applicable laws and regulations, and product characteristics at time of disposal.
Other hazards which do not result in classification
no data available
Handling and StoragePrecautions for safe handling
Handling in a well ventilated place. Wear suitable protective clothing. Avoid contact with skin and eyes. Avoid formation of dust and aerosols. Use non-sparking tools. Prevent fire caused by electrostatic discharge steam.
Conditions for safe storage, including any incompatibilities
Store the container tightly closed in a dry, cool and well-ventilated place. Store apart from foodstuff containers or incompatible materials.
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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Country Product Purchase Quantity Date Posted Post an enquiry for this product