GSK2850163 | CAS#2121989-91-9 | IRE1α inhibitor

MedKoo Cat#: 462577 | Name: GSK2850163

Featured

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity.

Chemical Structure

GSK2850163

CAS#2121989-91-9

Theoretical Analysis

MedKoo Cat#: 462577

Name: GSK2850163

CAS#: 2121989-91-9

Chemical Formula: C24H29Cl2N3O

Exact Mass: 445.1688

Molecular Weight: 446.42

Elemental Analysis: C, 64.57; H, 6.55; Cl, 15.88; N, 9.41; O, 3.58

Price and Availability

Size	Price	Availability
5mg	USD 285.00	2 Weeks
10mg	USD 500.00	2 Weeks
25mg	USD 950.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

GSK2850163; GSK 2850163; GSK-2850163; GSK163; GSK 163; GSK-163

IUPAC/Chemical Name

(R)-2-(3,4-dichlorobenzyl)-N-(4-methylbenzyl)-2,7-diazaspiro[4.5]decane-7-carboxamide

InChi Key

YFDASBFQKMHSSJ-XMMPIXPASA-N

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

SMILES Code

O=C(N(CCC1)C[C@]21CCN(CC3=CC=C(Cl)C(Cl)=C3)C2)NCC4=CC=C(C)C=C4

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.

In vitro activity:

TBD

In vivo activity:

The cardioprotective effect against I/R injury was also observed in the rat heart perfused with GSK2850163, a novel inhibitor of IRE1α. GSK2850163 improved LVSP (113.4±10.9 mmHg, p<0.01 vs. I/R), LVEDP (37.1±3.1mmHg, p<0.001 vs. I/R), LVDP (76.3±13.9 mmHg, p<0.001 vs. I/R), as well as +dp/dtmax (1586.5±263.3 mmHg/s, p<0.001 vs. I/R) and -dp/dtmax (-1127.7±159.9 mmHg/s, p<0.001 vs. I/R), which was associated with an inhibition of IRE1α phosphorylation (Figure 2A lower panel & Figure 2B). Reference: Int J Med Sci. 2022 Aug 15;19(9):1460-1472. https://pubmed.ncbi.nlm.nih.gov/36035373/

Preparing Stock Solutions

The following data is based on the product molecular weight 446.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Xue HM, Sun WT, Chen HX, He GW, Yang Q. Targeting IRE1α-JNK-c-Jun/AP-1-sEH Signaling Pathway Improves Myocardial and Coronary Endothelial Function Following Global Myocardial Ischemia/Reperfusion. Int J Med Sci. 2022 Aug 15;19(9):1460-1472. doi: 10.7150/ijms.74533. PMID: 36035373; PMCID: PMC9413556.

In vitro protocol:

TBD

In vivo protocol:

1: Nestor O. Concha, et al. Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity. Molecular Pharmacology December 2015, 88 (6) 1011-1023.