| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
GSK2850163 is a novel and potent inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which has IC50 values of 20 and 200 nM for IRE1α kinase and RNase activity, respectively. Activation of the inositol-requiring enzyme-1 alpha (IRE1a) protein caused by endoplasmic reticulum stress results in the homodimerization of the N-terminal endoplasmic reticulum luminal domains, autophosphorylation of the cytoplasmic kinase domains, and conformational changes to the cytoplasmic endoribonuclease (RNase) domains, which render them functional and can lead to the splicing of X-box binding protein 1 (XBP 1) mRNA.
| Targets |
IRE1α (IC50 = 20 nM); IRE1α (IC50 = 200 nM)
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|---|---|
| ln Vitro |
GSK2850163 is a new activator of inositol-requiring enzyme 1 alpha (IRE1α) that reduces RNase activity and IRE1α multiplication activity with IC50 values of 20 and 200 nM, respectively. In a dose-dependent way, GSK2850163 can lessen the rise in IRE1α autophosphorylation. GSK2850163 concentrations were able to raise the decreased activation of XBP 1. Ron (IC50=4.4 μM) and FGFR1 V561M (IC50=17 μM), two other mediators, are mildly inhibited by GSK2850163 [1].
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| References |
| Molecular Formula |
C24H29CL2N3O
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|---|---|
| Molecular Weight |
446.41256403923
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| Exact Mass |
445.17
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| Elemental Analysis |
C, 64.57; H, 6.55; Cl, 15.88; N, 9.41; O, 3.58
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| CAS # |
2121989-91-9
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| Related CAS # |
GSK2850163 (S enantiomer);2309519-81-9;GSK2850163 hydrochloride;2319838-09-8
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| PubChem CID |
73291790
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| Appearance |
Colorless to yellow solid powder
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| LogP |
4.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
583
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=CC=C(C=C1)CNC(=O)N2CCC[C@@]3(C2)CCN(C3)CC4=CC(=C(C=C4)Cl)Cl
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| InChi Key |
YFDASBFQKMHSSJ-XMMPIXPASA-N
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| InChi Code |
InChI=1S/C24H29Cl2N3O/c1-18-3-5-19(6-4-18)14-27-23(30)29-11-2-9-24(17-29)10-12-28(16-24)15-20-7-8-21(25)22(26)13-20/h3-8,13H,2,9-12,14-17H2,1H3,(H,27,30)/t24-/m1/s1
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| Chemical Name |
(5R)-2-[(3,4-dichlorophenyl)methyl]-N-[(4-methylphenyl)methyl]-2,7-diazaspiro[4.5]decane-7-carboxamide
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| Synonyms |
GSK2850163; GSK-2850163; GSK 2850163
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~67.5 mg/mL (~151.2 mM)
Ethanol: ~50 mg/mL (~112.0 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.25 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.25 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 22.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2401 mL | 11.2005 mL | 22.4009 mL | |
| 5 mM | 0.4480 mL | 2.2401 mL | 4.4802 mL | |
| 10 mM | 0.2240 mL | 1.1200 mL | 2.2401 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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