| Identification | Back Directory | [Name]
HG-9-91-01 | [CAS]
1456858-58-4 | [Synonyms]
HG-9-91-01
SIK INHIBITOR 1
1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-[6-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]urea
1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-(6-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)urea
N-(2,4-Dimethoxyphenyl)-N'-(2,6-dimethylphenyl)-N-[6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]urea
Urea, N-(2,4-dimethoxyphenyl)-N'-(2,6-dimethylphenyl)-N-[6-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]- | [Molecular Formula]
C32H37N7O3 | [MDL Number]
MFCD28167714 | [MOL File]
1456858-58-4.mol | [Molecular Weight]
567.68 |
| Chemical Properties | Back Directory | [Boiling point ]
790.8±60.0 °C(Predicted) | [density ]
1.257±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥56.8 mg/mL in DMSO; ≥27.3 mg/mL in EtOH; ≥6.35 mg/mL in H2O with ultrasonic | [form ]
Powder | [pka]
13.11±0.70(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
HG-9-91-01 is a potent and highly selective salt-inducible kinase (SIK) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3 respectively. | [Definition]
ChEBI: HG-9-91-01 is a member of the class of phenylureas that is a potent inhibitor of salt-inducible kinase 2, a potential target protein for therapy in ovarian cancer. It has a role as an antineoplastic agent and a salt-inducible kinase 2 inhibitor. It is a dimethoxybenzene, an aminopyrimidine, a N-arylpiperazine, a N-alkylpiperazine, a secondary amino compound and a member of phenylureas. | [Biological Activity]
hg-9-91-01 is a pan-sik (salt-inducible kinases) inhibitor with ic50 values of 0.92nm, 6.6nm and 9.6nm for sik1, sik2, sik3, respectively [1].siks restrict the formation of regulatory macrophages. the inhibition of these enzymes is thought to have potential for treating inflammatory and autoimmune diseases. hg-9-91-01 potently inhibits siks through targeting both the atp-binding site and the small hydrophobic pocket. it is reported that, besides siks, hg-9-91-01 also inhibits various protein tyrosine kinases such as src, btk, fgf and ephrin receptors. but other ampk-related kinase subfamily members are not sensitive to hg-9-91-01. hg-9-91-01 can promote lps-stimulated il-10 production, creb-dependent gene transcription, inhibit proinflammatory cytokine secretion and induce the expression of regulatory macrophage markers [1]. | [IC 50]
SIK1; SIK2; SIK3 | [storage]
Store at -20°C | [References]
[1] clark k, mackenzie k f, petkevicius k, et al. phosphorylation of crtc3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages. proceedings of the national academy of sciences, 2012, 109(42): 16986-16991. |
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