GSK2850163

SIGMA/SML1684 - ≥98% (HPLC)

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

CAS Number: 2121989-91-9
Empirical Formula (Hill Notation): C₂₄H₂₉Cl₂N₃O
Molecular Weight: 446.41
Linear Formula: C₂₄H₂₉Cl₂N₃O
Product Type: Chemical

Catalog Number	PKG Qty.	Price	Quantity


45-SML1684-5MG	5 mg	$119.00 1/EA		Add To Favorites
45-SML1684-25MG	25 mg	$480.00 1/EA		Add To Favorites

Properties
Descriptions
Safety Info.
Basic Data

assay	≥98% (HPLC)
color	colorless to light yellow
form	oil
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
InChI key	YFDASBFQKMHSSJ-XMMPIXPASA-N
Quality Level	100
SMILES string	ClC1=CC(CN(C2)CC[C@]32CN(C(NCC4=CC=C(C)C=C4)=O)CCC3)=CC=C1Cl
storage temp.	2-8°C

Biochem/physiol Actions:	GSK2850163 is a highly selective inhibitor of inositol requiring enzyme-1 alpha (IRE1α) with dual activity: it inhibits IRE1α kinase activity with an IC50 value of 20 nM and RNase activity with an IC50 value of 200 nM. IRE1α is a dual serine/threonine-protein kinase/endoribonuclease with two enzymatic domains: a trans-autophosphorylation domain and and endoribonuclease (RNase) domain. When activated, usually in response to endoplasmic reticulum (ER) stress such as the unfolded protein response (UPR), IRE1α oligomerizes and activates mRNA splicing of adaptive XBP1 transcription factor, which upregulates ER chaperones and ER associated degradation (ERAD) genes that promote degradation of ER unfolded proteins and facilitate recovery from ER stress. However, if ER stress is too high or chronic, IRE1α is hyperactivated, increasing many ER mRNAs, resulting in apoptosis. GSK2850163 interacts with IRE1α catalytic residues Lys599 and Glu612, displacing the kinase activation loop to the inactive DFG-out conformation. The rearrangement of the kinase domain-dimer interface also results in the RNAse domains rotating away from each other, inhibiting the RNase activity.
Biochem/physiol Actions:	IRE1α-selective inhibitor of XBP1 splicing
Biochem/physiol Actions:	IRE1α-selective inhibitor of XBP1 splicing. Homoharringtonine is a cephalotaxine ester that is also known as (HHT; 4-methyl (2R)-2-hydroxy-2-(4-hydroxy-4-methylpentyl)butanedioate). In gefitinib-resistant lung cancer cells, homoharringtonine promotes apoptosis and prevents signal transducer and activator of transcription (STAT3) through IL-6 (interleukin-6) /JAK1 (janus kinase 1)/STAT3 signal pathway. It plays an important role in the treatment of malaria.

Hazard statements	H413
RIDADR	NONH for all modes of transport
WGK Germany	WGK 3
Flash Point(F)	Not applicable
Flash Point(C)	Not applicable

Purity	≥98% (HPLC)
Storage Temp.	2-8°C
UNSPSC	12352200

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