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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC72097 SHR2415
SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer.
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DC72096 NIC-0102
NIC-0102 is an orally active proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammatory vesicle activation. NIC-0102 shows potent anti-inflammatory effects in a model of dextran sulfate sodium (DSS)-induced ulcerative colitis. NIC-0102 also inhibits production of pro-IL-1β.
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DC72095 Ac-WLA-AMC
Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate.
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DC72094 Ac-PAL-AMC
Ac-PAL-AMC is a fluorogenic substrate specific for 20S proteasome LMP2/β1i activity.
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DC72092 TVD-0003510
TVD-0003510 is a carboxamide derivative, and involves in synthesis of (2-((6-(2-aminopyrimidine-5-carboxamido)-8-methoxy-3,4-dihydro-2H-pyrimido[1,2-c]quinazolin-9-yl)oxy)ethyl)piperazine-l-carboxylate (C51), as a part of tert-butyl2-(4-hydroxyphenyl)acetate.
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DC72091 Piflufolastat
Piflufolastat (DCFPYL) can be used to the preparation of piflufolastat F 18 (DCFPyL F-18). piflufolastat F 18. Piflufolastat F-18 is an 18F-labelled diagnostic imaging agent. Piflufolastat F-18 can be used for positron emission tomography (PET) that targets prostate-specific membrane antigen (PSMA).
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DC72090 Imipramine pamoate
Imipramine pamoate is a potent anti-depressant compound.
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DC72089 FMF-06-098-1
FMF-06-098-1 is a highly multitargeted depressant. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.
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DC72088 Benzoquinoquinoxaline
Benzoquinoquinoxaline (BQQ) is a heterocyclic compound with an aminoalkyl side chain. Benzoquinoquinoxaline preferentially binds to DNA triplex structures, intercalates between the bases, thus, stabilising the triplex conformation. Conjugation of Benzoquinoquinoxaline to 1,10-phenanthroline specifically binds and cleaves double strand DNA at the site of formation of a triplex structure.
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DC72087 4-(Chloromethyl)-7-hydroxycoumarin
4-(Chloromethyl)-7-hydroxycoumarin (compound 4) is a hydroxycoumarin derivative with potent antioxidant effect and high hydroxyl radical-scavenging property. 4-(Chloromethyl)-7-hydroxycoumarin contains a methyl group and a chlorine group in the heterocyclic ring. A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties has been investigated as potent inhibitors of the zinc enzyme carbonic anhydrase, expecially tumor-associated isoforms CA IX and XII.
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DC72086 (R,1R)-Tenofovir amibufenamide
(R,1R)-Tenofovir amibufenamide ((R,1R)-HS-10234) can be used for the purifying a tenofovir prodrug. Tynofovir (tenofovir) is a nucleoside acids reverse transcriptase inhibitors.
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DC72085 Eplontersen
Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases.
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DC72084 Butabindide
Butabindide (UCL-1397) is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide inhibits TPP II to protect CCK-8 against inactivation.
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DC72083 (+)-EMD 57033
(+)-EMD 57033 is a cardiac troponin C (cTnC) activator, is a dominant Ca2+ sensitizer. (+)-EMD 57033 binds the cardiac/slow skeletal troponin C isoform and exerts myocardial contractile promotion function.
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DC72082 BLU2864
BLU2864 is an orally active, highly selective, ATP-competitive PRKACA inhibitor (IC50=0.3 nM). BLU2864 shows anti-tumor activity. BLU2864 can be used in cancer and polycystic kidney disease research.
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DC72079 SS-RJW100
SS-RJW100 is a enantiomer of RJW100, which is a racemic agonist of nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1). SS-RJW100 promotes recruitment of coregulator protein fragments in vitro, recruits the transcriptional intermediary factor 2 (Tif2) coactivator to LRH-1. SS-RJW100 diminishes LRH-1 allosteric activation networks, shows poor thermal stability.
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DC72078 DS01080522
DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer.
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DC72077 H1PVAT
H1PVAT is a potent and selective inhibitor of poliovirus serotypes (PV-1, PV-2, PV-3), and inhibits early stage of the replication. H1PVAT interacts with viral capsid directly and protects PV against heat inactivation.
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DC72075 AZ'6421
AZ'6421 acts as Protcolysis Targeting Chimera (PROTAC) to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer.
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DC72074 AM-1488
AM-1488 is a potent, orally active glycine receptor (GlyR) potentiator (hGlyRα3 EC50=0.45 μM).
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DC72073 Cidofovir diphosphate tri(triethylamine)
Cidofovir diphosphate tri triethylamine is an active intracellular metabolite of Cidofovir. Cidofovir diphosphate tri triethylamine is a selective inhibitor of viral DNA polymerases with Ki values of 6.6, 0.86 and 1.4 μM for HCMV, HSV-1 and HSV-2 DNA polymerase, respectively.
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DC72071 MAPTAM
MAPTAM is an intracellular Ca2+ chelator.
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DC72070 OX01914
OX01914 is a water-solube and permeable utrophin modulator (upregulates utrophin protein levels), with an EC50 of 20.5 μM. OX01914 can be used in study of duchenne muscular dystrophy (DMD).
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DC72069 4-Methylumbelliferyl oleate
4-Methylumbelliferyl oleate is a fluorogenic substrate for acid and alkaline lipases. 4-Methylumbelliferyl oleate is cleaved by lipases, liberating 4-Methylumbelliferyl (Ex/Em=320/450 nm).
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DC72068 1-Methylisatin
1-Methylisatin is a potent and selective CE (carboxylesterases) inhibitor, with Kis of 38.2 and 5.38 µM for hiCE and hCE1, respectively. 1-Methylisatin interacts with Hb (human adult hemoglobin) by hydrophobic binding and electrostatic attraction. 1-Methylisatin can be used in the study of regulation of drug metabolism in vivo.
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DC72067 Fluorescein diphosphate tetraammonium
Fluorescein diphosphate tetraammonium is a fluorescent dye, it can be used as a fluorogenic substrate and generats fluorescein as a fluorescent product.
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DC72065 C12 NBD Galactosylceramide
C12 NBD galactosylceramide, fluorescent dye, is a biologically active derivative of galactosylceramide that is tagged with a fluorescent C12 nitrobenzoxadiazole (C12 NBD) group. C12 NBD galactosylceramide can be used for the research of imaging.
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DC72064 PFM03
PFM03 is a MRE11 Endonuclease inhibitor. PFM03 regulates DNA double-strand break repair (DSBR) by nonhomologous end-joining (NHEJ).
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DC72063 Abacavir hydroxyacetate
Abacavir hydroxyacetate is an orally active inhibitor of IL-20 and PRINS. Abacavir hydroxyacetate reduces proliferation rate of skin in psoriasis as an immune modulator. Abacavir hydroxyacetate can be used for the research of inflammatory skin problems.
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DC72062 RR-RJW100
RR-RJW100, the enantiomer of RJW100, is an nuclear receptor liver receptor homolog 1 (LRH-1) and steroidogenic factor 1 (SF-1) agonist. RJW100 can be synthesized as two enantiomers, RR-RJW100 and SS-RJW100, with RR-RJW100 shown to be the more potent LRH-1 agonist. RR-RJW100 is involved in the regulation of metabolic homeostasis and is used in studies of diabetes, liver disease and inflammatory bowel disease.
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