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GPCR

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Cat. No. Product Name Field of Application Chemical Structure
DC80485 CRBN ligand-895
CRBN ligand-895 (Compound 14) is an E3 ubiquitin ligase ligand for cereblon (CRBN), which is used to recruit the cereblon protein. CRBN ligand-895 can be used for the synthesis of PROTACs, such as PROTAC HDAC8 Degrader-4.
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DC80460 ClpP activator-2
ClpP activator-2 (Compound GU18) is a ClpP activator with a Kd of 5.01 μM for HsClpP. ClpP activator-2 enhances the proteolytic activity of HsClpP and promotes the degradation of α-casein by HsClpP, with an EC50 of 1.09 μM. ClpP activator-2 induces the accumulation of mitochondrial reactive oxygen species (ROS), leading to damage to mitochondrial structure and function. ClpP activator-2 exhibits significant in vivo anti-multiple myeloma activity.
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DC80446 cis-3-(Aminomethyl)cyclobutanol hydrochloride
cis-3-(Aminomethyl)cyclobutanol hydrochloride is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC80405 CDK8-IN-2
CDK8-IN-2 is an orally active CDK8 inhibitor of an IC50 values of 0.010 μM. CDK8-IN-2 shows a CDK19 IC50 value of 0.026 μM. CDK8-IN-2 inhibits phospho-STAT1, a pharmacodynamic biomarker of CDK8. CDK8-IN-2 inhibits WNT pathway activity. CDK8-IN-2 can be used for the research of colorectal carcinoma.
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DC80377 CB1-receptor agonist-1
CB1-receptor agonist-1 is the racemic form of compound ‘1350 and is also a cannabinoid-1 receptor (CB1R) agonist.
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DC80374 Cathepsin C-IN-7
Cathepsin C-IN-7 (Page 68) is a Cathepsin C inhibitor. Cathepsin C-IN-7 can be used in research related to primary cancers and cancer metastases.
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DC80362 C20-Dihydrosphingomyelin
C20-Dihydrosphingomyelin (C20-DHSM; DHSM (d18:0/20:0)) is a saturated form of Sphingomyelin. C20-Dihydrosphingomyelin is a secondary component of most cell sphingolipids and its levels significantly decrease after intermittent fasting during Ramadan. C20-Dihydrosphingomyelin can be used for the development of liposome reagents.
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DC80360 C11-BODIPY 505/515 Glucosyl ceramide
C11-BODIPY 505/515 Glucosyl ceramide is a C11-BODIPY 505/515-labeled Glucosyl ceramide that can be used to prepare lipid nanoparticles for drug delivery (Ex/Em = 505/515 nm).
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DC80339 Br-C1-CONH-C5-CO-Val-Cit-PAB-MMAE
Br-C1-CONH-C5-CO-Val-Cit-PAB-MMAE (compound 62) is a drug-linker conjugate that contains a monomethyl auristatin E (MMAE) drug moiety, which is linked to a bromoacetamide-containing extension unit via a valine-citrulline (Val-Cit) dipeptide and a self-immolative p-aminobenzyl (PAB) spacer. Br-C1-CONH-C5-CO-Val-Cit-PAB-MMAE is applicable to the research of breast cancer, anaplastic large cell lymphoma and lung adenocarcinoma.
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DC80335 BR103354
BR103354 is an orally active, selective fibroblast activation protein (FAP) inhibitor with an IC50 value of 14 nM against hFAP. BR103354 restores the levels of phosphorylated ERK and Glut1 that are reduced by co-treatment with hFGF21 and FAP, decreases non-fasting blood glucose concentrations, improves glucose tolerance, and reduces hepatic triglyceride content. BR103354 ameliorates hepatic steatosis and hepatic fibrosis. BR103354 can be used in the research of type 2 diabetes and non-alcoholic steatohepatitis.
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DC80330 BODIPY TMR Lyso PA ester ammonium
BODIPY TMR Lyso PA ester ammonium is a lipid that can be used to prepare lipid nanoparticles (LNPs) for drug delivery.
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DC80245 AP-7-168
AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma.
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DC80239 Antitumor agent-214
Antitumor agent-214 is a chalcone analogue with anti-tumor activity. Antitumor agent-214 induces cell cycle arrest and apoptosis in tumor cells, disrupts mitochondrial metabolism, and upregulates the expression of caspase 3, caspase 7 and caspase 9, downregulates PARP1. Antitumor agent-214 can be used for anti-tumor research related to colorectal cancer, breast cancer, lung cancer, and cervical cancer.
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DC80225 Antioxidant 245
Antioxidant 245 (AO-245) is a hindered phenol antioxidant. Antioxidant 245 can be used in the research of nanocomposites.
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DC80194 Amonafide L-malate
Amonafide L-malate is a topoisomerase II inhibitor and DNA intercalator that induces Apoptotic signaling by blocking the binding of Topo II to DNA.
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DC80170 AK177
AK177 is an allosteric activator of IRE1α ribonuclease, with values of 480 nM and 180 nM against non-phosphorylated and phosphorylated IRE1α, respectively.\n
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DC80159 ADP receptor-IN-1
ADP receptor-IN-1 (compound 21) is a platelet ADP receptor inhibitor. ADP receptor-IN-1 shows both IC50 values <10 μM at a platelet ADP receptor binding assay and aggregation using a platelet-rich plasma assay.
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DC80132 9-Deoxyforskolin
9-Deoxyforskolin (compound 2) is a labdane-type diterpenoid, and also a forskolin derivative identified in hairy root cultures of Coleus forskohlii.
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DC80128 8-Oxo-Δ9-THC
8-Oxo-Δ9-THC is an oxygenated tetrahydrocannabinol that can be found in Cannabis sativa L. variety CHPF-01.
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DC80111 5-Hydroxymethyl flucloxacillin
5-Hydroxymethyl flucloxacillin is an active metabolite of Flucloxacillin. 5-Hydroxymethyl flucloxacillin exhibits antibacterial activity.
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DC80109 5-HT7/5-HT2A receptor antagonist 1
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity, orally active, brain-penetrant 5-HT7 and 5-HT2A receptor ligand having a pKi = 8.1 at both receptors. 5-HT7/5-HT2A receptor antagonist 1 behaves as an antagonist in an in vitro functional assay for 5-HT2A and as an inverse agonist in an in vitro functional assay for 5-HT7. 5-HT7/5-HT2A receptor antagonist 1 blockade of 5-Carboxamidotryptamine (5-CT) induced hypothermia in rats, and blockade of 2,5-dimethoxy-4-iodoamphetamine (DOI) induced head-twitches in mice. 5-HT7/5-HT2A receptor antagonist 1 occupied 5-HT2A receptor binding sites in the frontal cortex of the rat brain. 5-HT7/5-HT2A receptor antagonist 1 can be used for the study of Neurological diseases.
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DC80083 4-Guanidinobutanal
4-Guanidinobutanal is a nucleoside metabolite.
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DC80081 4-DMA-3'-OH-Chalcone
4-DMA-3'-OH-Chalcone (compound 24) is a synthetic chalcone derivative and selective cytotoxic agent.4-DMA-3'-OH-Chalcone reduces viability of endometriotic cells, while preserving or enhancing viability of eutopic endometrial cells.4-DMA-3'-OH-Chalcone can be used for the research of endometriosis.
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DC80088 4-Methoxyisophthalic acid
4-Methoxyisophthalic acid (4-Methoxy-1,3-benzenedicarboxylic acid) is a metal-organic framework (MOF).
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DC80012 1-Olein-2-butyrin-3-palmitin
1-Olein-2-butyrin-3-palmitin is an acylglycerol.
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DC79989 1954U89
1954U89 is a potent, lipid-soluble and orally active inhibitor of dihydrofolate reductase (DHFR). 1954U89 exhibits anticancer activity.
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DC79963 1,3-Linolenin-2-linolein
1,3-Linolenin-2-linolein is an acylglycerol.
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DC79951 1,2-Olein-3-acetyl
1,2-Olein-3-acetyl is an acylglycerol.
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DC79938 1-(2-(But-3-yn-1-yloxy)ethoxy)-6-chlorohexane
1-(2-(But-3-yn-1-yloxy)ethoxy)-6-chlorohexane is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC79934 (S,R,S,R)-AHPC-Me-CO-C7-N3
(S,R,S,R)-AHPC-Me-CO-C7-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S,R)-AHPC-Me based VHL ligand and a linker used in PROTAC technology. (S,R,S,R)-AHPC-Me-CO-C7-N3 can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-28.
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