DC Chemicals Limited
China
Product Name: SB216763
Price: $300.0/100mg $600.0/250mg $1200.0/1g
Purity: 98.0%
Stocking Period: 3 Day
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

280744-09-4

280744-09-4 structure

280744-09-4 structure

Name: SB216763
Chemical Name: 3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione
CAS Number: 280744-09-4
Molecular Formula: C₁₉H₁₂Cl₂N₂O₂
Molecular Weight: 371.217
Catalog: Biochemical Inhibitor PI3K/Akt/mTOR inhibitor (PI3K/Akt/mTOR) GSK-3 inhibitor
Create Date: 2018-12-03 07:49:17
Modify Date: 2024-01-02 20:06:16
SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.

Name	3-(2,4-dichlorophenyl)-4-(1-methylindol-3-yl)pyrrole-2,5-dione
Synonyms	3-(2,4-Dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione 1H-Pyrrole-2,5-dione, 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)- S1075_Selleck SB 216763 SB216763

Description	SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3 Signaling Pathways >> Stem Cell/Wnt >> GSK-3 Research Areas >> Neurological Disease
Target	GSK-3α:34.3 nM (IC50) GSK-3β:34.3 nM (IC50)
In Vitro	SB-216763 (10-20 µM) induces β-catenin mediated-transcription in a dose-dependent manner in HEK293 cells. SB-216763 (10, 15 and 20 µM) can maintain mESCs with a pluripotent-like morphology in long-term culture. SB-216763 (10 µM) can maintain J1 mESCs in a pluripotent state for more than a month[2]. SB-216763 inhibits GSK-3 with IC50 of 34 nM[3]. SB-216763 is equally effective at inhibiting human GSK-3α and GSK-3β[5].
In Vivo	SB216763 (20 mg/kg, i.v.) significantly improves the survival of BLM-treated mice. Mice randomized to receive BLM plus SB216763 shows a noteworthy reduction, compared with BLM-treated mice. SB216763 (20 mg/kg, i.v.) reduces the magnitude of BLM-induced alveolitis[1]. SB 216763 (0.2 mg/kg, i.v.) with either 17β-E100 or Geni100 reverses the ceiling effect because these agents significantly reduce infarct size when the rabbits' hearts are submitted to 30-min CAO[4].
Cell Assay	MESCs maintained with LIF or 10 µM SB-216763 for more than a month are resuspended at 40,000 cells/mL in LIF-free mESC medium. EBs are prepared by a hanging drop procedure. Briefly, 20 µL drops containing mESCs are pipetted on the inside of a 10-cm Petri dish lid. The lids are placed onto Petri dishes containing 10 mL of HBSS and the EBs are allowed to form and grow for 4 days in the incubator. After 4 days, 15-20 EBs are transferred to a well containing LIF-free mESC medium in a 24-well plate. The medium is exchanged every two days and autonomously beating cell aggregates are observed and counted.
Animal Admin	Mice are allocated to four groups (n=12/group) as follows: 1) intratracheal saline + vehicle (25% dimethyl sulfoxide, 25% polyethylene glycol, and 50% saline), 2) intratracheal saline + SB216763 (20 mg/kg) dissolved in vehicle, 3) intratracheal BLM (3 U/kg) + vehicle, and 4) intratracheal BLM + SB216763 (20 mg/kg) in vehicle. Another set of experiments to assess cytokine expression by reverse transcription-PCR is conducted in the mice (n=12/group) to receive 1) intratracheal saline + vehicle, 2) intratracheal BLM, and 3) intratracheal BLM + SB216763. To induce pulmonary fibrosis, BLM is intratracheally administered in mice (n=15/group) on day 0. BLM and saline-treated mice are administered with SB216763 dissolved in vehicle or vehicle alone intravenously at day 0 and then intraperitoneally twice a week until day 28. Mice are sacrificed by CO2 inhalation on days 2, 7, and 28. In the terminal deoxynucleotidyl transferase dUTP nick-end labeling (TUNEL) experiments, the cohorts of mice are as follows: saline-treated (n=6), BLM-treated (n=6), and BLM + SB216763-treated (n=6).
References	[1]. Gurrieri, et al. 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis. J.Pharmacol.Exp.Ther.2010 [2]. Kirby LA, et al. Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.PLoS One. 2012;7(6):e39329. Epub 2012 Jun 26. [3]. Wang M, et al. The first synthesis of [(11)C]SB-216763, a new potential PET agent for imaging of glycogen synthase kinase-3 (GSK-3).Bioorg Med Chem Lett. 2011 Jan 1;21(1):245-9. Epub 2010 Nov 11. [4]. The ceiling effect of pharmacological postconditioning with the phytoestrogen genistein is reversed by the GSK3beta inhibitor SB 216763 [3-(2,4-dichlorophenyl)-4(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione] through mitochondrial ATP-dependent potassium channel opening. [5]. Coghlan MP, et al. Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription. Chem Biol. 2000 Oct;7(10):793-803. [6]. Wang W, et al. Inhibition of glycogen synthase kinase 3beta ameliorates triptolide-induced acute cardiac injury by desensitizing mitochondrial permeability transition. Toxicol Appl Pharmacol. 2016 Dec 15;313:195-203.

Density	1.5±0.1 g/cm3
Boiling Point	598.1±50.0 °C at 760 mmHg
Melting Point	287-288.6ºC(lit.)
Molecular Formula	C₁₉H₁₂Cl₂N₂O₂
Molecular Weight	371.217
Flash Point	315.5±30.1 °C
Exact Mass	370.027588
PSA	51.10000
LogP	4.79
Appearance	orange
Vapour Pressure	0.0±1.7 mmHg at 25°C
Index of Refraction	1.702
Storage condition	−20°C
Water Solubility	DMSO: 20 mg/mL, soluble

Symbol	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: Irritant;
Risk Phrases	R36/37/38
Safety Phrases	26-36
RIDADR	NONH for all modes of transport
WGK Germany	3
HS Code	2933990090

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%