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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC40858 BSJ-04-132
BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity.
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DC40857 N-Acetylmuramic acid-alkyne
N-Acetylmuramic acid-alkyne is a derivative of N-acetylmuramic acid (NAM) component of bacterial peptidoglycans. N-Acetylmuramic acid-alkyne incorporates into bacterial peptidoglycans during biosynthesis. N-Acetylmuramic acid-alkyne can be used for fluorescent labeling of peptidoglycans when 'click'-conjugated to a fluorescent dye.
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DC40856 PM226
PM226 is a selective cannabinoid CB2R agonist (Ki (CB2R)=13 nM; EC50 (CB2R)=39 nM; Ki (CB1R) >40 μM;) with neuroprotective properties in vitro and vivo.
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DC40855 PSB 0777 ammonium
PSB 0777 ammonium is a potent and selective adenosine A2A receptor full agonist with Ki values of 44.4 nM, 360 nM for rat and human A2A receptors, respectively. PSB 0777 ammonium has Ki values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. PSB 0777 ammonium shows poor brain penetrant and perorally non-absorbable effect. PSB 0777 ammonium has the potential for inflammatory bowel disease (IBS) research research.
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DC40854 Cystathionine-γ-lyase-IN-1
Cystathionine-γ-lyase-IN-1 is a selective cystathionine γ-lyase (CSE) enzyme inhibitor with an IC50 of 6.3 μM.
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DC40853 SU5208
SU5208 inhibits vascular endothelial growth factor receptor-2 (VEGFR2).
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DC40852 TAN-452
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47?nM and a Kb of 0.21?nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56?nM and Kb=9.43?nM) and κ-opioid receptor (KOR; Ki=5.31?nM and Kb=7.18?nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.
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DC40851 TC-2559 difumarate
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 μM. Antinociceptive effect.
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DC40850 Sodium Glucoheptonate
Sodium Glucoheptonate is used as a kit for radio-labeling with Tc-99m. Tc-99m glucoheptonate is kidney- and brain-imaging agent, and can be used in brain-tumor detection.
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DC40845 UNC2399
UNC2399, a biotinylated UNC1999, is a selective EZH2 degrader, maintaining high in vitro potency for EZH2, with an IC50 of 17 nM.
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DC40844 (S,R,S)-AHPC-C5-NH2
(S,R,S)-AHPC-C5-NH2 (VH032-C5-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.
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DC40843 (S,R,S)-AHPC-C7-amine
(S,R,S)-AHPC-C7-amine (VH032-C7-amine) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used for estrogen-related receptor α (ERRα) PROTAC degrader.
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DC40842 Mal-amino-sulfo
Mal-amino-sulfo is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC40840 6-Maleimidocaproic acid sulfo-NHS
6-Maleimidocaproic acid sulfo-NHS is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC40839 Py-ds-dmBut-amido-PEG4-NHS ester
Py-ds-dmBut-amido-PEG4-NHS ester is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40838 Fmoc-NH-Azide-PEG4-L-Lysine-PFP ester
Fmoc-NH-Azide-PEG4-L-Lysine-PFP ester is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40837 Fmoc-Glu-(Boc)-Val-Cit-PAB-PNP
Fmoc-Glu-(Boc)-Val-Cit-PAB-PNP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40836 Mpro inhibitor N3 hemihydrate
Mpro inhibitor N3 hemihydrate is a potent inhibitor of SARS-CoV-2 Mpro with an EC50 of 16.77 μM for SARS-CoV-2. Mpro inhibitor N3 hemihydrate specifically inhibits Mpro from multiple coronaviruses, including SARS-CoV and MERS-CoV. Mpro inhibitor N3 hemihydrate displays inhibition against HCoV-229E, FIPV, and MHV-A59 with individual IC50 of 4.0 μM, 8.8 μM, and 2.7 μM, respectively.
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DC40835 DBCO-PEG3-propionic EVCit-PAB
DBCO-PEG3-propionic EVCit-PAB is a cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40834 Aldehyde-benzyl-PEG5-alkyne
Aldehyde-benzyl-PEG5-alkyne is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC40832 Azide-PEG1-Val-Cit-PABC-OH
Azide-PEG1-Val-Cit-PABC-OH is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40830 (2-pyridyldithio)-PEG1-hydrazine
(2-pyridyldithio)-PEG1-hydrazine is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40828 NHS-PEG2-SS-PEG2-NHS
NHS-PEG2-SS-PEG2-NHS is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40827 MC-VC-PAB-NH2
MC-VC-PAB-NH2 is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40826 NH2-PEG4-hydrazone-DBCO
NH2-PEG4-hydrazone-DBCO is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40825 N,N-Bis(PEG2-alkyne)-N-amido-PEG2-thiol
N,N-Bis(PEG2-alkyne)-N-amido-PEG2-thiol is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40824 N,N-Bis(PEG2-N3)-N-amido-PEG2-thiol
N,N-Bis(PEG2-N3)-N-amido-PEG2-thiol is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40823 ALD-PEG4-OPFP
ALD-PEG4-OPFP is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40822 BCOT-PEF3-OPFP
BCOT-PEF3-OPFP is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC40821 N1,N11-Diethylnorspermine tetrahydrochloride
N1,N11-Diethylnorspermine tetrahydrochloride (DENSPM tetrahydrochloride) potently induces SSAT (spermidine/spermine N1-acetyltransferase) mRNA and effectively stabilizes SSAT enzyme activity.
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