Name: NSC 23766 Trihydrochloride
Brand: Selleck Chemicals
SKU: S8031
Availability: InStock
Rating: 5 (107 reviews)

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Other Rho Inhibitors	EHop-016 ML141 (CID-2950007) CCG-1423 EHT 1864 2HCl ZCL278 MBQ-167 CCG-203971 Rhosin hydrochloride CID44216842 1A-116

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
RA4	Function Assay	50 μM	24 h		inhibits Matrigel invasion	17622308
RA3	Function Assay	50 μM	24 h		inhibits Matrigel invasion	17622308
RA2	Function Assay	50 μM	24 h		inhibits Matrigel invasion	17622308
RA1	Function Assay	50 μM	24 h		inhibits Matrigel invasion	17622308
RA-FLS (RA2)	Growth Inhibition Assay	25/50 μM	1-9 d		inhibits cell growth in both dose and time dependent manner	17622308
IEC-6	Function Assay	120 µM	4/6/8 h		prevents the increased activation of FAK at 6 and 8 h	20448461
MDA-MB-231	Function Assay	50/100 μM	48 h		induces a dose-dependent decrease in phosphorylation of p65 subunit	20515940
MDA-MB-468	Function Assay	50/100 μM	48 h		induces a dose-dependent decrease in phosphorylation of p65 subunit	20515940
MDA-MB-231	Function Assay	50/100 μM	24 h		increases phosphorylation of JNK in a dose dependent manner	20515940
MDA-MB-468	Function Assay	50/100 μM	24 h		increases phosphorylation of JNK in a dose dependent manner	20515940
MDA-MB-468	Function Assay	100 μM	24 h		inhibits caspase-3 activation	20515940
MDA-MB-468	Apoptosis Assay	50/100 μM	24 h		induces apoptosis	20515940
T47D	Function Assay	100 μM	48 h		increases the cell number in G1 phase and decreases the cell number in S and G2-M phases	20515940
MCF7	Function Assay	100 μM	48 h		increases the cell number in G1 phase and decreases the cell number in S and G2-M phases	20515940
MDA-MB-231	Function Assay	100 μM	48 h		increases the cell number in G1 phase and decreases the cell number in S and G2-M phases	20515940
MDA-MB-231	Function Assay	0-100 μM	24 h		selectively inhibits Rac1 activation without interfering with the activity of the closely related small GTPase Cdc42	20515940
MDA-MB-231	Cytotoxicity Assay	0-100 μM	48 h		decreases cell viability in a dose dependent manner	20515940
MDA-MB-468	Cytotoxicity Assay	0-100 μM	48 h		decreases cell viability in a dose dependent manner	20515940
T47D	Cytotoxicity Assay	0-100 μM	48 h		decreases cell viability in a dose dependent manner	20515940
MCF7	Cytotoxicity Assay	0-100 μM	48 h		decreases cell viability in a dose dependent manner	20515940
SKBR3-pMKO.1	Function Assay	50 μM	24 h		inhibits Rac1 activation	21943825
SKBR3	Function Assay	50 μM	24 h		inhibits Rac1 activation	21943825
NCI-H1703	Function Assay	0-500 μM	24 h		diminishes basal NF-κB activity dose dependently	22549160
NCI-H1703	Function Assay	100 μg/ml	24 h		slows progression through the G1 phase of the cell cycle	22549160
NCI-H1703	Growth Inhibition Assay	0-500 μM	24 h		inhibits cell growth in a dose dependent manner	22549160
T98MG	Function Assay	50 mM	24 h	DMSO	enhances the antimigratory effect of erlotinib	23832120
A172MG	Function Assay	50 mM	24 h	DMSO	enhances the antimigratory effect of erlotinib	23832120
U87MG	Function Assay	50 mM	24 h	DMSO	enhances the antimigratory effect of erlotinib	23832120
PC40	Cell Viability Assay	50 mM	144 h	DMSO	exhibits synergistic antiproliferative effects combined treatment with erlotinib	23832120
PC38	Cell Viability Assay	50 mM	144 h	DMSO	exhibits synergistic antiproliferative effects combined treatment with erlotinib	23832120
T98MG	Cell Viability Assay	50 mM	144 h	DMSO	exhibits synergistic antiproliferative effects combined treatment with erlotinib	23832120
A172MG	Cell Viability Assay	50 mM	144 h	DMSO	exhibits synergistic antiproliferative effects combined treatment with erlotinib	23832120
U87MG	Cell Viability Assay	50 mM	144 h	DMSO	exhibits synergistic antiproliferative effects combined treatment with erlotinib	23832120
Ki-67+ CLL	Growth Inhibition Assay	50 µM	5 d		decreases the number of Ki-67+ CLL cells	24501217
NIH3T3	Growth Inhibition Assay	100 μM	24 h		has no significant impact on cell viability	25037060
U2-OS	Function Assay	100 μM	24 h	DMSO	induces cell cycle arrest in the G1 phase	25109327
SW480	Function Assay	100 μM	24 h	DMSO	induces cell cycle arrest in the G1 phase	25109327
A431	Function Assay	100 μM	24 h	DMSO	induces cell cycle arrest in the G1 phase	25109327
U2-OS	Growth Inhibition Assay	100 μM	24/48/72 h		inhibits cell growth in a time dependent manner	25109327
SW480	Growth Inhibition Assay	100 μM	24/48/72 h		inhibits cell growth in a time dependent manner	25109327
A431	Growth Inhibition Assay	100 μM	24/48/72 h		inhibits cell growth in a time dependent manner	25109327
RBMECs	Function Assay	100 μM	30 min		blockes 6Bnz-cAMP-mediated activation of Rac1 in EMAP-II-treated RBMECs	26358039
human aortic smooth muscle cells	Function Assay	50 uM			Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 50 uM by SDS-PAGE based chemiluminescence	19527032
human aortic smooth muscle cells	Function Assay	100 μM			Inhibition of Rac1 binding to Pak1 in human aortic smooth muscle cells at 100 uM by SDS-PAGE based chemiluminescence	19527032
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 106 mg/mL (199.63 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 106 mg/mL

Ethanol : 5 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Chemical Information, Storage & Stability

Molecular Weight	530.97	Formula	C₂₄H₃₅N₇.3ClH	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1177865-17-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CCN(CC)CCCC(C)NC1=NC(=CC(=N1)NC2=CC3=C(C=C(N=C3C=C2)C)N)C.Cl.Cl.Cl

Mechanism of Action

Targets/IC₅₀/Ki	Rac GTPase (Cell-free assay) 50 μM
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%. [1] 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.
Kinase Assay	Rho GTPase activity assay
Kinase Assay	Cells are grown in log phase in a 10-cm dish, and are starved in 0.5% serum medium or indicated otherwise for 24 h before lysis in a buffer containing 20 mM Tris HCl (pH 7.6), 100 mM NaCl, 10 mM MgCl₂, 1% Nonidet P-40, 10% glycerol, and 1× protease inhibitor mixture. Lysates are clarified, the protein concentrations are normalized, and the GTP-bound Rac1 in the lysates is measured by an effector domain pull-down assay. For the His6-PAK1 PBD pull-down assay, cell lysates are incubated with Ni2+-agarose-immobilized His6-PAK1 PBD domain (∼1 μg each) purified from E. coli for 30 min. The Ni2+-agarose co-precipitates are washed twice in the wash buffer and analyzed by immunoblotting with anti-Rac1 monoclonal antibody.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15128949/ [2] https://pubmed.ncbi.nlm.nih.gov/16472687/ [3] https://pubmed.ncbi.nlm.nih.gov/16150730/ [4] https://pubmed.ncbi.nlm.nih.gov/18599867/ [5] https://pubmed.ncbi.nlm.nih.gov/20515940/ [6] https://pubmed.ncbi.nlm.nih.gov/21511011/

Applications

Methods	Biomarkers	Images	PMID
Western blot	pCREB / CREB OCT4 / SOX2 / Nanog active Rac1 / Rac1		25319697
Immunofluorescence	IP3K-A / F-actin BART / Rac1		19890013

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NSC 23766 Trihydrochloride Rac GTPase Inhibitor

Chemical Structure

Molecular Weight: 530.97