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HG-9-91-01 - 99%, high purity , CAS No.1456858-58-4, Inhibitor of salt inducible kinase 1;Inhibitor of salt inducible kinase 2;Inhibitor of SIK family kinase 3

COA COA
In stock
Item Number
H413999
Grouped product items
SKU Size
Availability
 Price Qty
H413999-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$197.90
H413999-25mg
25mg
3
$891.90
H413999-100mg
100mg
2
$1,335.90
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SIK Inhibitors

View related series
Immunology/Inflammation (1929) salt inducible kinase 1 Inhibitor (5) salt inducible kinase 2 Inhibitor (5) Salt-inducible Kinase (SIK) (15) SIK family kinase 3 Inhibitor (5)

Basic Description

Synonyms BCP25041 | DTXSID401025699 | SCHEMBL15271960 | SIK inhibitor 1 | HG-9-91-01 (1) | MS-30272 | 1-(2,4-Dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-(6-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-yl)urea | GTPL8049 | AKOS030526556 | NCGC00378591-01 | 1-(2
Specifications & Purity Moligand™, ≥99%
Biochemical and Physiological Mechanisms HG-9-91-01 (SIK inhibitor 1) is a potent and highly selective inhibitor of salt-inducible kinase (SIK) with IC50 of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3, respectively.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of salt inducible kinase 1;Inhibitor of salt inducible kinase 2;Inhibitor of SIK family kinase 3
Product Description

Information

HG-9-91-01 HG-9-91-01 (SIK inhibitor 1) is a potent and highly selective inhibitor of salt-inducible kinase (SIK) with IC50 of 0.92 nM, 6.6 nM and 9.6 nM for SIK1, SIK2 and SIK3, respectively.


Targets

SIK1 (Cell-free assay); SIK2 (Cell-free assay); SIK3 (Cell-free assay) 0.92 nM; 6.6 nM; 9.6 nM


In vitro

HG-9-91-01 is a potent and selective inhibitor of SIK. HG-9-91-01 not only targets the ATP-binding site, but also a small hydrophobic pocket adjacent to this site that is created by the presence of a small amino acid residue at this gatekeeper site. HG-9-91-01 inhibits a number of protein tyrosine kinases that possess a threonine residue at the gatekeeper site, such as Src family members (Src, Lck, and Yes), BTK, and the FGF and Ephrin receptors. HG-9-91-01 potently inhibits the SIKs and, crucially, does not inhibit any other member of the AMPK-related kinase subfamily, which all possess a large hydrophobic residue (Met or Leu) at the gatekeeper site. HG-9-91-01 increases LPS-stimulated IL-10 production and greatly suppressed proinflammatory cytokine secretion, even when cells are costimulated with IFNγ to generate fully polarized classically activated (M1) macrophages.


In vivo

HG-9-91-01 is > 99% serum bound and rapidly degraded by mouse liver microsomes (t1/2 = 11 min) making this compound unsuitable for direct injection into animals.


Cell Research(from reference)

Cell lines：Macrophages 

Concentrations：500 nM 

Incubation Time：1 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Diazinanes
Subclass Piperazines
Intermediate Tree Nodes Not available
Direct Parent Phenylpiperazines
Alternative Parents N-arylpiperazines  N-phenylureas  Dimethoxybenzenes  Methoxyanilines  m-Xylenes  Phenoxy compounds  Anisoles  Dialkylarylamines  Alkyl aryl ethers  Aminopyrimidines and derivatives  N-methylpiperazines  Imidolactams  Heteroaromatic compounds  Ureas  Trialkylamines  Azacyclic compounds  Hydrocarbon derivatives  Carbonyl compounds  Organic oxides  
Molecular Framework Aromatic heteromonocyclic compounds
Substituents Phenylpiperazine - N-arylpiperazine - N-phenylurea - M-dimethoxybenzene - Dimethoxybenzene - Methoxyaniline - Anisole - Phenoxy compound - Phenol ether - M-xylene - Xylene - Tertiary aliphatic/aromatic amine - Methoxybenzene - Aniline or substituted anilines - Dialkylarylamine - Alkyl aryl ether - Aminopyrimidine - N-methylpiperazine - N-alkylpiperazine - Imidolactam - Pyrimidine - Benzenoid - Monocyclic benzene moiety - Heteroaromatic compound - Urea - Tertiary aliphatic amine - Tertiary amine - Azacycle - Ether - Amine - Organic oxygen compound - Organonitrogen compound - Carbonyl group - Organooxygen compound - Organic nitrogen compound - Organic oxide - Hydrocarbon derivative - Aromatic heteromonocyclic compound
Description This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
External Descriptors Not available

Product Properties

ALogP 6.214
hba_count 5
HBD Count 2
Rotatable Bond 8

Associated Targets(Human)

SIK1 Tchem Serine/threonine-protein kinase SIK1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
SIK2 Tchem Serine/threonine-protein kinase SIK2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
SIK3 Tchem Serine/threonine-protein kinase SIK3 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK3 Tchem Serine/threonine-protein kinase MST2 (3069 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK4 Tchem Serine/threonine-protein kinase MST1 (2643 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PAK1 Tchem Serine/threonine-protein kinase PAK 1 (2601 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK24 Tchem Serine/threonine-protein kinase 24 (980 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SIK1 Tchem Serine/threonine-protein kinase SIK1 (1440 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SIK2 Tchem Serine/threonine-protein kinase SIK2 (1467 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK26 Tchem Serine/threonine-protein kinase MST4 (1915 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SIK3 Tchem Serine/threonine-protein kinase SIK3 (566 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504772435
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504772435
IUPAC Name 1-(2,4-dimethoxyphenyl)-3-(2,6-dimethylphenyl)-1-[6-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]urea
INCHI InChI=1S/C32H37N7O3/c1-22-7-6-8-23(2)31(22)36-32(40)39(27-14-13-26(41-4)19-28(27)42-5)30-20-29(33-21-34-30)35-24-9-11-25(12-10-24)38-17-15-37(3)16-18-38/h6-14,19-21H,15-18H2,1-5H3,(H,36,40)(H,33,34,35)
InChIKey UYUHRKLITDJEHB-UHFFFAOYSA-N
Smiles CC1=C(C(=CC=C1)C)NC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC=NC(=C3)NC4=CC=C(C=C4)N5CCN(CC5)C
Isomeric SMILES CC1=C(C(=CC=C1)C)NC(=O)N(C2=C(C=C(C=C2)OC)OC)C3=NC=NC(=C3)NC4=CC=C(C=C4)N5CCN(CC5)C
Molecular Weight 567.68
Reaxy-Rn 24079892
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24079892&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

2 results found

Lot Number Certificate Type Date Item
G2221203 Certificate of Analysis May 09, 2025 H413999
G2221218 Certificate of Analysis May 09, 2025 H413999

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 100 mg/mL (176.15 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility 100
DMSO(mM) Max Solubility 176.155580608794
Water(mg / mL) Max Solubility ＜1
Molecular Weight 567.700 g/mol
XLogP3 5.300
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 8
Rotatable Bond Count 8
Exact Mass 567.296 Da
Monoisotopic Mass 567.296 Da
Topological Polar Surface Area 95.100 Ų
Heavy Atom Count 42
Formal Charge 0
Complexity 825.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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