CRT0036521

  Cat. No.:  DC60005   Featured
Chemical Structure
327092-81-9
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
More than 5000 active chemicals with high quality for research!
Field of application
CRT0036521 is a potent and selective inhibitor of AKR1C3.
Cas No.: 327092-81-9
Chemical Name: 3-((3,4-Dihydroisoquinolin-2(1H)-yl)sulfonyl)benzoic acid
Synonyms: 3-((3,4-Dihydroisoquinolin-2(1H)-yl)sulfonyl)benzoic acid;3-(3,4-dihydro-1H-isoquinolin-2-ylsulfonyl)benzoic acid;3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic acid;3-(3,4-Dihydroisoquinolin-2(1H)-ylsulphonyl)benzoic acid;006075;3-(2-1,2,3,4-tetrahydroisoquinolylsulfonyl)benzoic acid;3-(3,4-Dihydro-1H-isoquinoline-2-sulfonyl)-benzoic acid;AC1LEIZA;AC1Q73IW;CHEMBL1566492;SBB002606;ZERO
SMILES: C1C2C(=CC=CC=2)CCN1S(C1=CC=CC(C(O)=O)=C1)(=O)=O
Formula: C16H15NO4S
M.Wt: 317.35960316658
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO Application
Description: CRT0036521(AKR1C3-IN-1) is a potent, highly selective inhibitor of AKR1C3, with an IC50 of 13 nM.
Target: IC50: 13 nM (AKR1C3)[1]
In Vitro: AKR1C3-IN-1 shows less potent activities with 20.3±3.8 μM against AKR1C1 and >30 μM against AKR1C2 and AKR1C4. AKR1C3-IN-1 inhibits AKR1C3 activity (inhibiting PR-104H formation) with an IC50 of 0.027±0.002 μM[1].
Kinase Assay: A competitive fluorescence assay is used to measure AKR1C enzyme activity, where a nonfluorescent ketone probe (probe 5) selective for the AKR1C enzyme isoforms is reduced to a fluorescent alcohol in the presence of AKR1C enzyme and NADPH. Briefly, purified protein (2 μg/mL AKR1C1, 1 μg/mL AKR1C2, 2 μg/mL AKR1C3, and 5 μg/mL AKR1C4) are incubated with 40 μM probe 5, AKR1C3-IN-1, and 50 μM NADPH in an assay buffer of 10 mM MOPS (pH=7.2), 130 mM NaCl, 1 mM DTT, and 0.01% Triton-X-100 for 1 h at 37°C. The reaction is stopped by addition of 35 mM NaOH, and fluorescence is read in a SpectraMax M2 microplate reader at excitation/emission wavelengths of 420/510 nM. The compounds and known AKR1C3 inhibitors (flufenamic acid, indomethacin, naproxen, meclofenamic acid, S(+)-ibuprofen and flurbiprofen) are tested at multiple concentrations between 0.1 nM and 100 μM in 2% DMSO to generate AKR1C enzyme inhibition data. Compound IC50 values are calculated by fitting the inhibition data to a four-parameter logistic sigmoidal dose-response curve using Prism 5.02.
References: [1]. Jamieson SM, et al. 3-(3,4-Dihydroisoquinolin-2(1H)-ylsulfonyl)benzoic Acids: highly potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. J Med Chem. 2012 Sep 13;55(17):7746-58.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC33635 DODAP DODAP, also known as 1,2-Dioleoyl-3-dimethylammonium-propane, is a cationic lipid. It has been used as a component in liposomes that can be used to encapsulate siRNA, immunostimulatory oligodeoxynucleotides, antisense oligonucleotides, or chemotherapeutic agents for in vitro and in vivo delivery.
DC58047 DSPE-PEG 2000 PEG2000-DSPE is used for creating micelles that are able to carry drugs with low solubility.
DC31000 LP-01 LP-01 is an ionizable cationic amino lipid (pKa = ~6.1). It has been used in the generation of lipid nanoparticles (LNPs). LNPs containing LP-01 and encapsulating both Cas9 mRNA and modified single-guide RNA (sgRNA) for the transport protein transthyretin (Ttr) induce gene editing in liver cells in mice in a dose-dependent manner resulting in reduced serum Ttr levels for at least 12 months.
DC66546 R-Sirpiglenastat R-Sirpiglenastat is the R- isomer of Sirpiglenastat(DRP-104).Sirpiglenastat (DRP104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.
DC60597 AZD0780 AZD0780 is the first oral small molecule PCSK9 inhibitor for the treatment of hypercholesterolemia.
DC66114 FAPI-46 FAPI46 is a quinoline-based fibroblast activation protein (FAP)-targeted radiotracer. FAPI-46 has higher tumor uptake and prolonged tumor accumulation. FAPI 46 can be used for tumor imaging of a multitude of different cancers.
DC60580 Endosidin5(ES5) Endosidine 5 (ES5), is one of the most potent small molecules interferes with recycling endosomes through Annexin A6, thereby promoting the release and expression of mRNA into the cytoplasm. The delivered mRNAs is greatly enhanced via inhibition of endocytic recycling in cells and in live mice. NAV2729 (NAV) and endosidin 5 (ES5), resulted in significant enhancement (1.5–2 folds) of LNP-mediated delivery of Fluc mRNAs. Incubation of NAV and ES5 together caused modest further increases in Fluc expression in comparison to the sole application of either compound.
DC90056 PLX-5622 HCl form (water solubility form) PLX5622 is the HCl salt form of PLX-5622, which has better water solubility.PLX-5622 is a highly selective brain-penetrant CSF1R inhibitor (IC50=0.016 µM; Ki=5.9 nM) allowing for extended and specific microglial elimination, preceding and during pathology development.
DC60559 PT-179 PT-179 is a new orthogonal immunomodulatory drug (IMiD) derivative that binds CRBN but does not induce degradation of off-target proteins. PT-179 potently degrades proteins fused to SD40 at either the N or C terminus.
DC65841 MC1 MC1 is a selective and potent inhibitor for COX-2, and [11C]MC1 detected COX-2 in nonhuman primates after intracerebral injection of an inflammogen.
X