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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC28305 FAPy-adenine
FAPy-adenine is an oxidized DNA base. Fapy-adenine shows an increased trend levels in the Alzheimer's disease brain. Oxidized nucleosides are biochemical markers for tumors, aging, and neurodegenerative diseases.
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DC28304 7α-Hydroxy-4-cholesten-3-one
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1.
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DC28303 Allotetrahydrocortisol
Allotetrahydrocortisol (5a-Tetrahydrocortisol) is a metabolite of Cortisol. Cortisol is the main glucocorticoid in human. It is produced in adrenal cortex and plays a crucial role in many physiological processes.
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DC28302 Tetrahydrocortisone
Tetrahydrocortisone is a stress-induced hormone. Tetrahydrocortisone is also a urinary metabolite of Cortisone derived from the reduction of Cortisone by 5-reductase.
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DC28301 Cysteinylglycine TFA
Cysteinylglycine TFA is an endogenous metabolite and used in disease diagnosis.
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DC28300 Mevalonic acid lithium salt
Mevalonic acid lithium salt, a precursor in the mevalonate pathway, is essential for cell growth and proliferation.
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DC28299 L-hydroxylysine dihydrochloride
L-hydroxylysine dihydrochloride ((2S,5R)-5-Hydroxylysine dihydrochloride), an amino acid, is exclusive to collagen protein, which is formed by posttranslational hydroxylation of some lysine residues.
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DC28297 Sparfosic acid trisodium
Sparfosic acid trisodium, is a potent inhibitor of aspartate transcarbamoyl transferase, with anti-tumor and antimetabolite activity. Aspartate transcarbamoyl transferase catalyzes the second step of de novo pyrimidine biosynthesis.
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DC28296 V-9302 hydrochloride
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
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DC28294 Bis-PEG1-PFP ester
Bis-PEG1-PFP ester is a non-cleavable (1 unit PEG) ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28293 Bis-PEG2-PFP ester
Bis-PEG2-PFP ester is also a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Bis-PEG2-PFP ester is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC28291 Carnostatine hydrochloride
Carnostatine hydrochloride (SAN9812 hydrochloride) is a potent and selective carnosinase 1 (CN1) inhibitor with a Ki of 11 nM for human recombinant CN1. Carnostatine hydrochloride can be used for the treatment of diabetic nephropathy (DN).
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DC28289 HAMI 3379
HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT2) receptor antagonist. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury, and attenuates microglia-related inflammation.
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DC28288 XL-784 free base
XL-784 free base is a selective matrix metalloproteinases (MMP) inhibitor, with IC50s of ~1900, 0.81, 120, 10.8, 18, 0.56 nM for MMP-1,MMP-2,MMP-3,MMP-8,MMP-9,MMP-13,respectively.
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DC28287 (R)-CSN5i-3
(R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.
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DC28286 2-Selenouracil
2-Selenouracil is a useful specialized photosensitizer for photodynamical therapy.
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DC28285 NUCC-390
NUCC-390 is a novel and selective small-molecule CXCR4 receptor agonist. NUCC-390 can induce internalization of CXCR4 receptors.
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DC28284 (S)-IDO1-IN-5
(S)-IDO1-IN-5 (Example 1B) is an active S-isomer of IDO1-IN-5. (S)-IDO1-IN-5 binds to IDOL with an IC50 value less than 1.5 µΜ. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
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DC28283 (Rac)-IDO1-IN-5
(Rac)-IDO1-IN-5 (Example 1) is a racemate of IDO1-IN-5. IDO1-IN-5 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1.
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DC28282 (3R,4R)-A2-32-01
(3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
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DC28281 DBCO-NHCO-PEG4-NHS ester
DBCO-NHCO-PEG4-NHS ester ester is a MMP-2- and cathepsin B- (CatB) cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28280 c(phg-isoDGR-(NMe)k) TFA
c(phg-isoDGR-(NMe)k) TFA is a selective and potent α5β1-integrin ligand with an IC50 of 2.9 nM.
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DC28279 RTI-118
RTI-118 is a novel small-molecule neuropeptide S receptor (NPSR) antagonist. RTI-118 can relieve drug addiction including selectively decrease cocaine self-administration.
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DC28276 GSK1702934A
GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
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DC28275 BIP-135
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.
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DC28274 CU-T12-9
CU-T12-9 is a specific TLR1/2 agonist with EC50 of 52.9 nM in HEK-Blue hTLR2 SEAP assay. CU-T12-9 activates both the innate and the adaptive immune systems. CU-T12-9 selectively activates the TLR1/2 heterodimer, not TLR2/6. CU-T12-9 signals through NF-κB and invokes an elevation of the downstream effectors TNF-α, IL-10, and iNOS.
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DC28273 ML334
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
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DC28272 CINPA1
CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC50 of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function.
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DC28268 Pregnenolone monosulfate sodium salt
Pregnenolone monosulfate sodium salt (3β-Hydroxy-5-pregnen-20-one monosulfate sodium salt) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone monosulfate sodium salt acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone monosulfate sodium salt can protect the brain from cannabis intoxication.
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DC28265 DSR-6434
DSR-6434 is a potent and selective Toll-like receptor 7 (TLR7) agonist, with EC50s of 7.2 nM and 4.6 nM for human and mice TLR7, respectively. DSR-6434 has a strong antitumor effect.
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