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Safety Information

SML2718

Sigma-Aldrich

GSK503

≥98% (HPLC)

Synonym(s):

GSK 503, GSK-503, N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-3-methyl-6-(6-(4-methylpiperazin-1-yl)pyridin-3-yl)-1H-indole-4-carboxamide, N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-methyl-1-(1-methylethyl)-6-[6-(4-methyl-1-piperazinyl)-3-pyridinyl]-1H-indole-4-carboxamide

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1 EA
CN¥1,118.65

CN¥1,118.65

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About This Item

Empirical Formula (Hill Notation):
C31H38N6O2
CAS Number:
1346572-63-1
Molecular Weight:
526.67
MDL number:
MFCD28405142
UNSPSC Code:
12352200
NACRES:
NA.77

CN¥1,118.65

Please contact Customer Service for Availability
Request a Bulk Order

Quality Level

100

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

[nH]1[c](c(c(cc1C)C)CNC(=O)c2c3c([n](cc3C)C(C)C)cc(c2)c4cnc(cc4)N5CCN(CC5)C)=O

InChI

1S/C31H38N6O2/c1-19(2)37-18-21(4)29-25(30(38)33-17-26-20(3)13-22(5)34-31(26)39)14-24(15-27(29)37)23-7-8-28(32-16-23)36-11-9-35(6)10-12-36/h7-8,13-16,18-19H,9-12,17H2,1-6H3,(H,33,38)(H,34,39)

InChI key

HRDQQHUKUIKFHT-UHFFFAOYSA-N

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Anti-IP3 Receptor 1 Antibody serum, from rabbit

071213

Anti-IP3 Receptor 1 Antibody

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Anti-IP3 Receptor 1 Antibody Chemicon®, from rabbit

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Anti-IP3 Receptor 2 Antibody serum, Chemicon®

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Anti-IP3 Receptor 2 Antibody

antibody form

serum

antibody form

serum

antibody form

affinity purified immunoglobulin

antibody form

serum

species reactivity

mouse, human

species reactivity

mouse, rat, human

species reactivity

rat

species reactivity

human, mouse

clone

polyclonal

clone

polyclonal

clone

polyclonal

clone

polyclonal

shipped in

wet ice

shipped in

wet ice

shipped in

wet ice

shipped in

wet ice

Gene Information

dog ... Itpr1(476548)
human ... ITPR1(3708)
mouse ... Itpr1(16438)
rat ... Itpr1(25262)

Gene Information

human ... ITPR3(3710)
mouse ... Itpr3(16440)
rat ... Itpr3(25679)

Gene Information

human ... ITPR1(3708)

Gene Information

human ... ITPR2(3709)

Biochem/physiol Actions

GSK503 is a potent and selective histone-lysine N-methyltransferase EZH2 (ENX1, KMT6) inhibitor (IC50/Kiapp = 8/3 nM/EZH2, 27 nM/Y641C, <5 nM/A677G, Y641F/H/N/S EZH2 mutants vs. 633/636 nM/EZH1) with >4,000-fold selectivity over other histone methyltransferases and little potency toward panels of histone acetylases/deacetylases, kinases, GPCR/channels/transporters. GSK503 reduces splenocyte H3K27me3 level and prevents post immunization germinal center (GC) formation (150 mg/kg/day i.p.; mice) with good pharmacokinetics in vivo. GSK503 abrogates the GC hyperplasia phenotype of Ezh2(Y641N) mice and suppresses human DLBCL xenografts tumor growth in mice.
Potent and selective histone-lysine N-methyltransferase EZH2 (ENX1, KMT6) inhibitor in vitro and in vivo. Displays >200-fold selectivity over EZH1.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000089675
0000089676
0000081070

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Loredana Puca et al.
Nature communications, 9(1), 2404-2404 (2018-06-21)
A major hurdle in the study of rare tumors is a lack of existing preclinical models. Neuroendocrine prostate cancer is an uncommon and aggressive histologic variant of prostate cancer that may arise de novo or as a mechanism of treatment
Michael D Onken et al.
Science signaling, 11(546) (2018-09-06)
Constitutively active G protein α subunits cause cancer, cholera, Sturge-Weber syndrome, and other disorders. Therapeutic intervention by targeted inhibition of constitutively active Gα subunits in these disorders has yet to be achieved. We found that constitutively active Gαq in uveal
Marc-Werner Dobenecker et al.
The Journal of experimental medicine, 215(4), 1101-1113 (2018-03-11)
Differentiation and activation of T cells require the activity of numerous histone lysine methyltransferases (HMT) that control the transcriptional T cell output. One of the most potent regulators of T cell differentiation is the HMT Ezh2. Ezh2 is a key
Wendy Béguelin et al.
Nature communications, 8(1), 877-877 (2017-10-14)
The EZH2 histone methyltransferase is required for B cells to form germinal centers (GC). Here we show that EZH2 mediates GC formation through repression of cyclin-dependent kinase inhibitor CDKN1A (p21Cip1). Deletion of Cdkn1a rescues the GC reaction in Ezh2 -/-
Daniel Zingg et al.
Cancer cell, 34(1), 69-84 (2018-07-17)
Human melanomas frequently harbor amplifications of EZH2. However, the contribution of EZH2 to melanoma formation has remained elusive. Taking advantage of murine melanoma models, we show that EZH2 drives tumorigenesis from benign BrafV600E- or NrasQ61K-expressing melanocytes by silencing of genes

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