Wedelolactone - ≥98%(HPLC), high purity , CAS No.524-12-9, Inhibitor of CBR1

Item Number
W124219
Grouped product items
SKUSizeAvailabilityPrice Qty
W124219-1mg
1mg
In stock
$20.90
W124219-5mg
5mg
In stock
$86.90
W124219-25mg
25mg
Available within 4-8 weeks(?)
Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!
$391.90

Selective and irreversible IκB kinase inhibitor

View related series
CBR1 Inhibitor

Basic Description

Synonyms7-Methoxy-5,11,12-trihydroxycoumestan | 7-Methoxy-5,11,12-trihydroxy-coumestan | IKK Inhibitor II | NCGC00163667-01 | BRD-K53635676-001-02-3 | 1,8,9-Trihydroxy-3-methoxycoumestan | CS-0009079 | DTXSID60200408 | 1,8,9-Trihydroxy-3-methoxy-6H-[1]benzofuro[3
Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsWedelolactone inhibits NF-κB-mediated gene transcription in cells by blocking the phosphorylation and degradation of IκBα. Irreversible inhibitor of IKKα and β kinase activity (IC50 < 10 μM). Wedelolactone has no effects on p38 MAP kinase or Akt.Selective
Storage TempStore at 2-8°C
Shipped InWet ice
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of CBR1
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Wedelolactone, a compound originally extracted from Eclipta alba, has been shown to inhibit caspase-11, which is a key regulator of proinflammatory cytokine IL-1β maturation and pathological apoptosis. Mechanistic studies suggest that caspase-11 is inhibited by reduction of NF-κB-mediated transcription. Furthermore, this compound has been shown to inhibit IKKγ, a kinase that is crucial for activation of NF-κB, as well as IKK α and IKK β. Weldelolactone also displays potent trypsin inhibition capacities. Additional studies suggest that Wedelolactone contains antagonistic properties towards two PLA2 myotoxins that were isolated from Agkistrodon contortix laticinctus and Crotalus virdis virdis. This agent has also been noted to contain antihepatotoxic behavior consequentially protecting primary cultured liver cells from the toxicity of CC14, Phalloidin, and galactosamine, and inhibit 5-lipoxygenase (5-LO)) activity in porcine leukocytes.
Inhibits caspase-11; a key regulator of proinflammatory cytokine IL-1β maturation and apoptosis.

Associated Targets(Human)

CBR1 Tchem Carbonyl reductase [NADPH] 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ALOX5 Tclin Arachidonate 5-lipoxygenase (6568 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
VDR Tclin Vitamin D receptor (26531 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ACHE Tclin Acetylcholinesterase (18204 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
THRB Tclin Thyroid hormone receptor beta-1 (7926 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DAPK3 Tchem Death-associated protein kinase 3 (2108 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK11 Tchem MAP kinase p38 beta (2785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K6 Tchem Dual specificity mitogen-activated protein kinase kinase 6 (1284 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1G1 Tchem Casein kinase I gamma 1 (2496 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK2B Tchem CaM kinase II beta (1626 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK6 Tclin Cyclin-dependent kinase 6 (1724 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHEK2 Tchem Serine/threonine-protein kinase Chk2 (4015 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDPK1 Tchem 3-phosphoinositide dependent protein kinase-1 (3758 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKAA2 Tchem AMP-activated protein kinase, alpha-2 subunit (1328 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHUK Tchem Inhibitor of nuclear factor kappa B kinase alpha subunit (3170 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
IKBKB Tchem Inhibitor of nuclear factor kappa B kinase beta subunit (5554 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIM1 Tchem Serine/threonine-protein kinase PIM1 (9629 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PLK1 Tchem Serine/threonine-protein kinase PLK1 (28605 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK4 Tbio CaM kinase IV (2116 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 (1262 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTK2 Tclin Focal adhesion kinase 1 (4730 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK2D Tchem CaM kinase II delta (2813 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1G2 Tchem Casein kinase I gamma 2 (2539 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAPK3 Tchem MAP kinase ERK1 (4725 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PRKACA Tchem cAMP-dependent protein kinase alpha-catalytic subunit (3475 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK2A Tchem CaM kinase II alpha (1938 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RPS6KA3 Tchem Ribosomal protein S6 kinase alpha 3 (4284 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NFKBIA Tchem NF-kappaB inhibitor alpha (187 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PLK4 Tchem Serine/threonine-protein kinase PLK4 (1882 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
STK16 Tchem Serine/threonine-protein kinase 16 (910 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
STK10 Tchem Serine/threonine-protein kinase 10 (2119 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK1 Tchem Dual specificty protein kinase CLK1 (2189 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK2 Tchem Dual specificity protein kinase CLK2 (3942 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CLK3 Tchem Dual specificity protein kinase CLK3 (2711 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK2 Tchem Serine/threonine-protein kinase NEK2 (3514 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK16 Tchem Serine/threonine-protein kinase PCTAIRE-1 (829 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
STK4 Tchem Serine/threonine-protein kinase MST1 (2643 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK1D Tchem CaM kinase I delta (2141 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMK1G Tchem CaM kinase I gamma (570 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CAMKK2 Tchem CaM-kinase kinase beta (1281 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAP3K5 Tchem Mitogen-activated protein kinase kinase kinase 5 (1965 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLK Tchem Serine/threonine-protein kinase 2 (1640 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NEK6 Tchem Serine/threonine-protein kinase NEK6 (1986 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PAK6 Tchem Serine/threonine-protein kinase PAK6 (1915 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PIM2 Tchem Serine/threonine-protein kinase PIM2 (5873 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PAK5 Tchem Serine/threonine-protein kinase PAK7 (1760 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
STK17A Tchem Serine/threonine-protein kinase 17A (1791 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TNIK Tchem TRAF2- and NCK-interacting kinase (1174 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Camk2g CaM kinase II gamma (1 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hepatitis C virus (23859 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GCN5 Histone acetyltransferase GCN5 (89 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BCHE Cholinesterase (8742 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rorc Nuclear receptor ROR-gamma (89407 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
fba Putative fructose-1,6-bisphosphate aldolase (15559 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ffp 4'-phosphopantetheinyl transferase ffp (24982 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
FTL Ferritin light chain (43324 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
stx1 Shiga toxin 1 variant A subunit (37 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
resT Telomere resolvase resT (23 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Gabrp GABA-A receptor; anion channel (5731 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
stx1 Shiga toxin (517 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 1,8,9-trihydroxy-3-methoxy-[1]benzofuro[3,2-c]chromen-6-one
INCHI InChI=1S/C16H10O7/c1-21-6-2-10(19)14-12(3-6)23-16(20)13-7-4-8(17)9(18)5-11(7)22-15(13)14/h2-5,17-19H,1H3
InChi Key XQDCKJKKMFWXGB-UHFFFAOYSA-N
Canonical SMILES COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O
Isomeric SMILES COC1=CC(=C2C(=C1)OC(=O)C3=C2OC4=CC(=C(C=C43)O)O)O
WGK Germany 3
PubChem CID 5281813
Molecular Weight 314.25

Certificates

Certificate of Analysis(COA)

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Lot NumberCertificate TypeDateItem
E1525108Certificate of AnalysisFeb 06, 2023 W124219

Chemical and Physical Properties

SolubilitySoluble in DMSO (25 mg/mL), and MeOH.
SensitivityHeat Sensitive
Melt Point(°C)315 °C

Safety and Hazards(GHS)

Pictogram(s) GHS07
Signal Warning
Hazard Statements

H302:Harmful if swallowed

H317:May cause an allergic skin reaction

Precautionary Statements

P261:Avoid breathing dust/fume/gas/mist/vapors/spray.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352:IF ON SKIN: wash with plenty of water.

P321:Specific treatment (see ... on this label).

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P270:Do not eat, drink or smoke when using this product.

P272:Contaminated work clothing should not be allowed out of the workplace.

P333+P313:IF SKIN irritation or rash occurs: Get medical advice/attention.

P362+P364:Take off contaminated clothing and wash it before reuse.

P330:Rinse mouth.

P301+P317:IF SWALLOWED: Get medical help.

WGK Germany 3

Related Documents

Citations of This Product

1. Du Si-Hao, Qiao Dong-Fang, Chen Chuan-Xiang, Chen Si, Liu Chao, Lin Zhoumeng, Wang Huijun, Xie Wei-Bing.  (2017)  Toll-Like Receptor 4 Mediates Methamphetamine-Induced Neuroinflammation through Caspase-11 Signaling Pathway in Astrocytes.  Frontiers in Molecular Neuroscience,  10  (409).  [PMID:29311802] [10.3389/fnmol.2017.00409]

References

1. Du Si-Hao, Qiao Dong-Fang, Chen Chuan-Xiang, Chen Si, Liu Chao, Lin Zhoumeng, Wang Huijun, Xie Wei-Bing.  (2017)  Toll-Like Receptor 4 Mediates Methamphetamine-Induced Neuroinflammation through Caspase-11 Signaling Pathway in Astrocytes.  Frontiers in Molecular Neuroscience,  10  (409).  [PMID:29311802] [10.3389/fnmol.2017.00409]

Solution Calculators