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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC78303 dRRM-1
dRRM-1 is a DCAF15-dependent molecular glue degrader of RBM39 and RBM23. dRRM-1 can rescue the self-degradation of DCAF15. dRRM-1 can be used for the research of cancer.
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DC78302 BWD
BWD is a PSMA ligand (IC50 = 35.86). BWD exhibits excellent in vitro stability and high affinity. BWD can enhance tumor uptake and retention. BWD can inhibit tumor growth in vivo. BWD can be studied in anticancer research.
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DC78301 BIRB-1017
BIRB-1017 is a potent inhibitor of p38 MAP kinase. BIRB-1017 can be used in inflammation research.
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DC78300 PQM-244
PQM-244 (Compound 5c) is an orally active and multi-target modulator of TRPV1 and CB1 and CB2 receptors. PQM-244 has significant peripheral antinociceptive effects on both neurogenic and inflammatory phases. PQM-244 also has potential antioxidant activity with an IC50  of  14.15 µM for radical scavenging DPPH. PQM-244 can be used for chronic pain and inflammatory disease research, such as diabetes, atherosclerosis and Alzheimer’s disease.
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DC78299 4-Hydroxy xylazine O-glucuronide lithium
4-Hydroxy xylazine O-glucuronide (lithium) is a metabolite of the α2-adrenergic receptor agonist xylazine. 4-Hydroxy xylazine O-glucuronide (lithium) can be synthesized from xylazine via the intermediate metabolite 4-hydroxy xylazine.
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DC78298 ECC-5004
ECC-5004 (Compound 1) is a GLP-1 receptor agonist with an EC50 of 0-20 nM. ECC-5004 exhibits strong inhibitory effects on OATP1B1, with an IC50 < 1 μM. ECC-5004 can be used to study diseases such as diabetes, obesity, and non-alcoholic fatty liver disease.
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DC78297 Satoprodil
Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC50 value of 123 nM for NR2B.
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DC78296 TRIM25 ligand-1
TRIM25 ligand-1 (Compound 10) is a covalent ligand. TRIM25 ligand-1 can covalently bind to Cys498 in the PRYSPRY domain of TRIM25 and enhance its auto-ubiquitination activity. TRIM25 ligand-1 is selective for TRIM25 in vitro and in live cells.
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DC78295 dAPM-1 acetate
dAPM-1 (acetate) is a peptidomimetic antibiotic agent. dAPM-1 (acetate) can selectively induces intracellular aggregation in B. subtilis. dAPM-1 (acetate) is active against S. aureus, methicillin-resistant S. aureus (MRSA), B. subtilis, E. faecium, and M. smegmatis with MICs of 8, 4, 4, 8, and 16 µg/ml, respectively.
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DC78294 (3S,4R)-ME-344
(3S,4R)-ME-344 is the (3S,4R)-enantiomer of ME-344). ME-344 is a mitochondrial Heme oxygenase 1 (HO-1) inhibitor. ME-344 specifically binds and alters HO-1 structure, and increases HO-1 translocation from the rough endoplasmic reticulum to mitochondria, but only in drug-sensitive cells (such as H460 and SHP-77 cells). ME-344 decreases mitochondrial ATP production and induces ROS, with subsequent disruption of redox homeostasis and mitochondrial function. ME-344 has significant antitumor activity, and can be used for cancers like breast cancer research.
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DC78293 YTHDF2 ligand-1
YTHDF2 ligand-1 (Compound 23) is a selective and high-affinity YTHDF2 ligand with a Kd of 1.3 μM (FP assay) and an IC50 of 11 μM (HTRF assay) . YTHDF2 ligand-1 can be used in the study of cancer.
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DC78292 MS44
MS44 is a potent aurora kinase B (AURKB PROTAC) degrader (DC50 = 103 nM). MS44 effectively degrades AURKB in a time- and ubiquitin-proteasome system (UPS)-dependent manner and is selective for AURKB over AURKA and AURKC. MS44 effectively inhibits the proliferation in multiple cancer cell lines and potently induces G2/M arrest. MS44 can be used for the study of AURKB-dependent tumors.
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DC78291 Debio 1453
Debio 1453 is a bactericidal FabI inhibitor potent against N. gonorrhoeae (IC50 = 0.6 nM), including drug-resistant strains. Debio 1453 demonstrates a low propensity for resistance selection and is effective in eradicating both planktonic and intracellular bacteria through a mechanism of concurrently inhibiting FabI and engaging the non-mutable NADH cofactor. Debio 1453 clears antibiotic-resistant N. gonorrhoeae infection in a murine vaginal model. Debio 1453 can be used for gonorrhoea research.
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DC78290 14-3-3σ/ERα stabilizer-2
14-3-3σ/ERα stabilizer-2 (Compound 41) is a covalent 14-3-3σ/ERα stabilizer with a Kd of 10.1 nM. 14-3-3σ/ERα stabilizer-2 significantly decreases the dissociation rate of ERα, stabilizing the binary ERα/14-3-3σ interaction. 14-3-3σ/ERα stabilizer-2 can be used for molecular glues research.
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DC78289 AU-461
AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM). AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers.
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DC78288 HUP-46
HUP-46 is a BBB-penatrable modulator of αSyn dimerization and autophagy. HUP-46 reduces the ratio of pPP2A/PP2A, increases the autophagy marker LC3BII levels, and decreases αSyn dimerization. HUP-46 can be used for research of neurodegenerative diseases.
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DC78287 1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc
1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc is a phospholipid-porphyrin conjugate. 1-Palmitoyl-2-pyropheophorbide a-sn-glycero-3-pc can be utilized in photodynamic therapy research.
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DC78286 ONO-9517601
ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders.
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DC78285 ONO-7927846
ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders.
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DC78284 MJ-26
MJ-26 is an inhibitor targeting Menin. MJ-26 has high binding affinity (Ki: 0.56 μM) and significant antiproliferative activity. MJ-26 works by inhibiting Menin-MLL interaction and inducing Menin protein degradation. MJ-26 has significant antitumor effects on acute myeloid leukemia (AML). MJ-26 can be used in AML research.
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DC78283 FLT3/JAK2/BRD4 ligand-1
FLT3/JAK2/BRD4 ligand-1 is a FLT3/JAK2/BRD4 ligand. FLT3/JAK2/BRD4 ligand-1 can be used for synthesis PROTAC FLT3/JAK2/BRD4 Degrader-1.
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DC78282 AAG561
AAG561 is a corticotropin-releasing factor receptor 1 (CRF1) antagonist. AAG561 can be used for the study of the underlying emotion dysregulation of a mental disease or disorder.
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DC78281 Deutaleglitazar
Deutaleglitazar (Aleglitazar-d2) is a agonist of dual peroxisome proliferatory activating receptor (PPARα and PPARγ).
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DC78280 AF151
AF151 is a METTL3 PROTAC degrader with the DC50 of 0.43 μM in MOLM-13 cells. AF151 inhibits cell growth by significantly degrading METTL3 protein and reducing m6A levels. AF151 can induce cell apoptosis and reduce the level of Bcl-2 protein. AF151 can be used for research on cancer such as acute myeloid leukemia (AML).
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DC78279 (S,R,S)-AHPC-CO-C2-phenylboronic acid
(S,R,S)-AHPC-CO-C2-phenylboronic acid is an E3 ligase ligand-linker conjugate that incorporates the VH032-based VHL ligand and linker. (S,R,S)-AHPC-CO-C2-phenylboronic acid can be used for synthesis of PROTAC AF151.
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DC78278 IA107
IA107 is a potent, selective, and allosteric IRE1α RNase (IC50 = 16 nM (non phosphorylated), IC50 = 9 nM (phosphorylated)) inhibitor. IA107 can inhibit endoplasmic reticulum stress-induced XBP1 mRNA splicing and protein expression, and has no cytotoxicity.
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DC78277 FB231
FB231 is a Parkin activator. FB231 can induce mild mitochondrial stress, resulting in impaired mitochondrial function and activation of the integrated stress response. FB231 can lower the threshold for mitochondrial toxins to induce PINK1/Parkin-mediated mitophagy. FB231 can cause activation of the integrated stress response (ISR) and perturbation to iron-dependent pathways. FB231 can be used for the research of neurological disease, such as Parkinson’s disease.
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DC78276 ML-93
ML-93 is an orally active SAE inhibitor, with an IC50 value of 0.4 μM. ML-93 inhibits the SUMOylation pathway in HCT116 cells. ML-93 shows robust antitumor activity in the HCT116 colorectal carcinoma xenograft model. ML-93 can be used for the study of colorectal cancer.
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DC78275 VU6002703
VU6002703 (Compound 17) is a BBB-penetrable M4 mAChR positive allosteric modulator (PAM) with an EC50 of 0.6  μM for hM4. VU6002703 can be used for neuropsychiatric and rare genetic CNS disorders research.
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DC78274 CPI-203-PEG1-C3-O-COOH
CPI-203-PEG1-C3-O-COOH is a conjugate of the BRD4 ligand and the linker. CPI-203-PEG1-C3-O-COOH can be used for synthesizing PROTAC BRD4 degrader ARV-771
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