YKL-05-099( YKL 05-099 )

Catalog No. M13037 CAS No. 1936529-65-5

COA

Datasheet

HNMR

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Product Name

YKL-05-099
Note

Research use only, not for human use.
Brief Description

YKL-05-099 (YKL 05-099) is a novel potent, selective pan-SIK inhibitor with IC50 of 10, 40 and 30 nM for SIK1, 2 and 3, respectively.
Description

YKL-05-099 (YKL 05-099) is a novel potent, selective pan-SIK inhibitor with IC50 of 10, 40 and 30 nM for SIK1, 2 and 3, respectively; displays increased SIK selectivity and enhanced pharmacokinetic properties compared with HG-9-91-01; reduces LPS stimulated phosphorylation of HDAC5 at the SIK-specific phosphorylation site Ser259, increases expression of the CREB target genes Il10 and Nurr77, suppresses production of TNFα, IL-6 and IL-12p40 in BMDMs; a useful probe to investigate SIK function in vivo.
In Vitro

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In Vivo

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Synonyms

YKL 05-099
Pathway

Autophagy
Target

SIK
Recptor

SIK
Research Area

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Indication

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CAS Number

1936529-65-5
Formula Weight

600.11046
Molecular Formula

C32H34ClN7O3
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 103.33 mg/mL; PBS: 100 mM
SMILES

O=C1N(C2=NC=C(OC)C=C2)C3=NC(NC4=CC=C(C5CCN(C)CC5)C=C4OC)=NC=C3CN1C6=C(C)C=CC=C6Cl
Chemical Name

Pyrimido[4,5-d]pyrimidin-2(1H)-one, 3-(2-chloro-6-methylphenyl)-3,4-dihydro-7-[[2-methoxy-4-(1-methyl-4-piperidinyl)phenyl]amino]-1-(5-methoxy-2-pyridinyl)-

1. Sundberg TB, et al. ACS Chem Biol. 2016 Aug 19;11(8):2105-11. 2. Wein MN, et al. Nat Commun. 2016 Oct 19;7:13176.

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