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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC77505 FLAC6
FLAC6 is a potent fluorinated detergent that can be used to solubilize membrane proteins (the native adenosine receptor A2AR, a G protein-coupled receptor, and two native transporters AcrB and BmrA). FLAC6 can maintain the structural and functional integrity of different membrane proteins.
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DC77504 Filipin II
Filipin II is an antibiotic, which exhibits antifungal efficacy. Filipin II interacts with membrane sterols, leads to changes in membrane structure, inhibits Candida utilis and Saccharomyces cerevisiae with the MIC of 0.03 mg/L and 0.2 μg/L.
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DC77503 FCOB02
FCOB02 is a monoamine oxidase B (MAO-B) ligand. FCOB02 can be labeled as [18F]FCOB02, a 4-methylcoumarin-like targeting probe. [18F]FCOB02 has a high affinity for MAO-B with an IC50 of 10.68 nM. [18F]FCOB02 can be used in specific MAO-B imaging as well as quantitative analysis in vivo.
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DC77502 FAPI-FUSCC-07
FAPI-FUSCC-07 is a targeted probe for fibroblast activation protein (FAP), exhibiting high affinity binding to FAP for applications in molecular imaging, tumor diagnosis, and radiotherapy.
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DC77501 FAP targeting peptide-PEG2 conjugate
FAP targeting peptide-PEG2 conjugate (Example A1) is the peptide and linker conjugate of Unlabeled FXX489. Unlabeled FXX489 is a fibroblast activation protein (FAP)-targeting ligand.
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DC77500 FAP targeting peptide for FXX489
FAP targeting peptide for FXX489 is the polypeptide part of Unlabeled FXX489. Unlabeled FXX489 is a fibroblast activation protein (FAP)-targeting ligand.
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DC77499 Ethanolamine-Thalidomide-4-OH
Ethanolamine-Thalidomide-4-OH is an E3 Ligase Ligand-Linker Conjugate composed of an CRBN ligand and a linker, and can be used for synthesis of PROTACs.
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DC77498 Erythromycin propionate
Erythromycin propionate, erythromycin derivative, is a macrolide antibiotic used in the treatment of a wide variety of bacterial infections. Erythromycin propionate causes several cases of liver injury which mostly include cholestatic hepatitis. Erythromycin propionate toxicity is related to its inhibitory effect on bile acid transport.
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DC77497 epi-D-Captopril
epi-D-Captopril (epi-D-SQ 14225) is a stereoisomer of Captopril and an inhibitor of metallo-β-lactamases (MBLs). The IC50 values of epi-D-Captopril against NDM-1, IMP-1, and VIM-2 are 64 μM, 173 μM, and 5.5 μM, respectively. epi-D-Captopril is expected to be used in the research of diseases caused by MBLs-related drug-resistant bacterial infections.
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DC77496 EP-3945
EP-3945 is a potent agonist of Mas-related G protein-coupled receptor (MRGPR), more effective than the MRGPRD small molecule agonist β-Alanine. MRGPR plays a crucial role in inflammatory pruritus and pain sensation. Additionally, MRGPR binds to Gq (MRGPRX2, MRGPRX4, MRGPRX1 couple with Gq; MRGPRX2, MRGPRD couple with Gi), with EP-3945 measured EC50 for Gq being 211.6 nM.
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DC77495 endo-BCN-PEG2-NHS ester
endo-BCN-PEG2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. endo-BCN-PEG2-NHS ester contains a BCN group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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DC77494 EN1441
EN1441 is a covalent degrader targeting the androgen receptor (AR) with an EC50 value of 4.2 μM and its truncated variant AR-V7. EN1441 selectively and potently degrades both AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 is promising for research of androgen-independent prostate cancers.
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DC77493 EB-TCIP
EB-TCIP (BAK-04-212) is a bivalent molecule comprised of AP1867 and BI-3812. EB-TCIP can form a reversible ternary complex between FKBPF36V and BCL6BTB. EB-TCIP recruits FKBP12F36V-tagged EWS/FLI1 to DNA sites bound by the transcriptional regulator BCL6, leading to rapid expression of BCL6 target genes (eg: SOCS2 and CXCL11). EWS/FLI1 is a fusion transcription factors in Ewing sarcoma. EB-TCIP can be used for research of deregulated transcription in cancer.
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DC77492 E197
E197 is the inhibitor for DOCK5 that destroys the podosome belt structure of osteoclasts, thereby inhibiting the bone resorption (IC50=3.44 μM in human osteoclast). E197 inhibits the Rac in DOCK5 expressing HEK293 cell with an IC50 of 36 μM. E197 prevents the bone loss in mouse ovariectomized models.
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DC77491 DS-1150b
DS-1150b is an orally active GLUT4 activator. DS-1150b has the activity of activating GLUT4 transport and can promote the translocation of GLUT4 to the cell membrane in skeletal muscle cells. DS-1150b has shown hypoglycemic effects in the Zucker obese rat model and can be used in the study of type 2 diabetes mellitus (T2DM).
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DC77490 DPM-1003
DPM-1003 is a PTP1B conformational inhibitor that targets the non-catalytic, disordered segment at the C-terminus of the PTP1B protein, showing improvement in lung inflammation in mice.
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DC77489 DOTA-NI-FAPI-04
DOTA-NI-FAPI-04 is a FAP inhibitor (IC50 = 7.44 nM). By integrating FAP targeting with hypoxia-sensitive groups (nitroimidazole), DOTA-NI-FAPI-04 significantly enhances tumor uptake and retention capabilities. DOTA-NI-FAPI-04 chelates metallic isotopes (such as 68Ga and 177Lu) through DOTA to produce radioactive probes ([68Ga]Ga/DOTA-NI-FAPI-04 and [177Lu]Lu/DOTA-NI-FAPI-04), which can be used for research in tumor diagnostics and therapeutic agents. DOTA-NI-FAPI-04 holds dual targeting potential in the fields of cancer imaging, tumor microenvironment analysis, and radionuclide therapy, particularly suitable for scenarios where the tumor stroma and hypoxic regions synergistically interact.
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DC77488 DOTAGA-FAP-2286-ALB
DOTAGA-FAP-2286-ALB is a derivative of Rofapitide tetraxetan. m3227G(
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DC77487 Donepezil N-oxide
Donepezil N-oxide, a metabolite of Donepezil. Ogerin analogue 1 is generally used as a negative control.
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DC77486 Docosapentaenoic acid (22n-3) sodium
Docosapentaenoic acid (22n-3) sodium is a component of phospholipids. Docosapentaenoic acid 22n-3 sodium has inhibitory activity against α-amylase and α-glucosidase, with IC50s value of 17 μg/mL and 22 μg/mL, respectively. Docosapentaenoic acid 22n-3 sodium increases cell vitality. Docosapentaenoic acid 22n-3 sodium has a weak anti-inflammatory effect.
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DC77485 DNJ-20
DNJ-20 is an α-glucosidase inhibitor (IC50: 55.3 μg/mL). DNJ-20 has broad-spectrum anti-SARS-CoV-2 activity. DNJ-20 inhibits the correct processing of viral glycoproteins by interfering with the endoplasmic reticulum-associated glycoprotein folding process (ERQC), thereby blocking the formation and infection of viral particles. DNJ-20 has IC50 values up to 1.49 uM against several SARS-CoV-2 variants, as well as HCoV-229E and HCoV-0C43。DNJ-20 can be used for pan-coronavirus research.
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DC77484 DM21-L-G
DM21-L-G is a Drug-Linker Conjugates that can be used to synthesize ADC molecules.
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DC77483 DL5055
DL5055 (compound 6k) is a potent and selective hCAR activator with an EC50 of 0.35 μM. DL5055 induces CYP2B6 expression and hCAR nuclear translocation in human primary hepatocytes.
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DC77482 DL-01 TFA
DL-01 TFA is the TFA salt form of DL-01. GSK-364735 potassium is an antiretroviral, that inhibits the integrase of human immunodeficiency virus type 1 (HIV-
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DC77481 Dihydroxyacetone phosphate dilithium
Dihydroxyacetone phosphate dilithium (DHAP) is used for studies of fructose metabolism, trioses and glycosylation. Dihydroxyacetone phosphate dilithium is used for studies involving the metabolism of trisaccharide pools and their roles in physiological and physical processes.
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DC77480 Diclofenac amide
Diclofenac amide is a prodrug for Diclofenac sodium. Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan-induced rat paw edema model without causing gastric ulcer (300 μmol/kg).
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DC77479 Desthiazolylmethyl ritonavir
Desthiazolylmethyl ritonavir is a base-catalyzed degradation product of the HIV protease inhibitor Ritonavir, black: linker, Blue: E3 ligase ligand).
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DC77478 DEL-I25
DEL-I25 is a potent GPX4 activator. DEL-I25 protects cells from ferroptosis.
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DC77477 DEG-35
DEG-35 is a CRBN-dependent, dual IKZF2 and CK1α molecule glue degrader, with DC50 values of 1.4 nM and 4.4 nM for CK1α and IKZF2, respectively. DEG-35 activates the p53 apoptosis pathway. DEG-35 can be used in the research for Acute Myeloid Leukemia (AML).
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DC77476 Defactinib analogue-1
Defactinib analogue-1 (Compound 7) is a ligand for target protein Fak, that can be used for synthesis of PROTAC FAK degrader 1. 11(Z),14(Z)-Eicosadienoic acid ethanolamide inhibits the inactivating transport of an endogenous cannabinoid substance with an IC50 value of 10.6 μM. 11(Z),14(Z)-Eicosadienoic acid ethanolamide can be used for research of neuropsychiatric conditions.
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