AKR1C3 Inhibitor I

• Catalog number
  2403-5
• Price
  Please ask
• Size
  5 mg

• Alternative_name
  3-(3,4-Dihydroisoquinolin2(1H)-ylsulfonyl)benzoic acid
• Description
  A highly potent and selective inhibitor of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. In repeat assays it showed an IC₅₀ of 0.013 ± 0.003 μM for AKR1C3, compared with 20.3 ± 3.8 μM against AKR1C1 and >30 μM against AKR1C2 and AKR1C4. This inhibitor also showed displays potency in a cellular assay, blocking the ability of AKR1C3 to metabolize a proven substrate. Does not display any COX (cyclooxygenase) inhibition at 10 µM in whole blood assay.
• Structure Available
  Yes
• Peptide sequence
  No
• Salt Form
  No
• Molecular Formula
  C₁₆H₁₅NO₄S
• Molecular Weight
  317.36
• Cell Permeable
  Yes
• Purity
  ≥98% by HPLC
• Solubilities
  DMSO
• Handling
  Protect from air and light
• Tag Line
  A potent and selective AKR1C3 inhibitor
• Storage Condition
  -20°C
• Shipping Condition
  gel pack
• Shelf Life
  36 months
• SMILES
  O=S(C1=CC(C(O)=O)=CC=C1)(N2CCC(C=CC=C3)=C3C2)=O
• InChi
  InChI=1S/C16H15NO4S/c18-16(19)13-6-3-7-15(10-13)22(20,21)17-9-8-12-4-1-2-5-14(12)11-17/h1-7,10H,8-9,11H2,(H,18,19)
• InChi Key
  ZGVIUMKHTXKKOX-UHFFFAOYSA-N
• Data Sheet Link
• MSDS Available
  Yes
• Additional description
  Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.

• Gene target
  AKR1C3   Inhibitor  
• Gene symbol
  AKR1C3
• Short name
  AKR1C3 Inhibitor I
• Alternative name
  aldo-keto reductase family 1, member complement component 3 (3-a hydroxysteroid dehydrogenase, classification II) suppressor I
• Alternative to gene target
  aldo-keto reductase family 1, member C3 (3-alpha hydroxysteroid dehydrogenase, type II), DD3 and DDX and HA1753 and HAKRB and HAKRe and hluPGFS and HSD17B5 and PGFS, AKR1C3 and IDBG-47964 and ENSG00000196139 and 8644, oxidoreductase activity, nuclei

Gene info

• Identity
  HGNC:386
• Gene
  AKR1C3
• Long gene name
  aldo-keto reductase family 1 member C3
• Synonyms gene
  • HSD17B5
• Synonyms gene name
  • hydroxysteroid (17-beta) dehydrogenase 5
  • aldo-keto reductase family 1, member C3 (3-alpha hydroxysteroid dehydrogenase, type II)
• Synonyms
  • KIAA0119
  • DDX
  • HAKRB
  • PGFS
• Synonyms name
  • dihydrodiol dehydrogenase X
  • prostaglandin F synthase
  • 3-alpha hydroxysteroid dehydrogenase, type II
• GenBank acession
  • L43839
• Locus
  10p15.1
• Discovery year
  1998-09-29
• Entrez gene record
  8644
• Pubmed identfication
  • 7650035
  • 9792917
• RefSeq identity
  • NM_003739
• Classification
  • Aldo-keto reductases
• VEGA ID
  OTTHUMG00000017585

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