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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC78694 MTP3 ligand-1
MTP3 ligand-1 is a MTP3 ligand for PROTAC MTP3 degrade-1. PROTAC MTP3 degrade-1 is a PROTAC based MYC degrader.
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DC78693 MTP3 Ligand-linker Conjugate 1
MTP3 Ligand-linker Conjugate 1 is a conjugate of the MTP3 ligand and the linker. MTP3 Ligand-linker Conjugate 1 can be used for synthesis of PROTAC MTP3 degrade-1.
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DC78692 CRBN ligand-186
CRBN ligand-186 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
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DC78691 BBH-4
BBH-4 is a SARS-CoV-2 major protease (MPro) inhibitor. BBH-4 can be used in SARS-CoV-2 infection research.
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DC78690 Trabectedin derivative 1 TFA
Trabectedin derivative 1 TFA is a selective DNA minor groove binder. Trabectedin derivative 1 TFA inhibits DNA transcription and repair to induce tumor cell apoptosis. Trabectedin derivative 1 TFA is promising for research of solid tumors such as soft tissue sarcoma and ovarian cancer.
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DC78689 BION106
BION106 is a dihydrofolate reductasethymidylate synthase (DHFR-TS) PROTAC degrader. BION106 exhibits extremely strong anti-malarial activity with a Ki and toxicity of 2.68 nM and 0.2 μM against Plasmodium falciparum, and > 100 μM and 44.2 μM in mammalian cells. BION106 can be used for the study of antimalarial parasites.
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DC78688 PSMA-DIM
PSMA-DIM is a dimeric PSMA ligand with a Kd of 37.09 nM for LNCaP cells. PSMA-DIM can be radiolabeled with [68Ga]Ga to form [68Ga]Ga-PSMA-DIM. [68Ga]Ga-PSMA-DIM can effectively distinguish between cells and animal models with different expression levels of PSMA. [68Ga]Ga-PSMA-DIM exhibits high LNCaP cells uptake and tumor uptake peak values. PSMA-DIM can be used for the study of prostate cancer (PCa).
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DC78687 DCB29
DCB29 is a selective inhibitor of the BPTF bromodomain, with an IC50 value of 13.2 μM. DCB29 can be used for the study of the treatment of BPTF-related diseases (such as bladder cancer, colorectal cancer, melanoma, leukemia, and other cancers).
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DC78686 Antitumor photosensitizer-9
Antitumor photosensitizer-9 is a near-infrared Photosensitizer (PS) with a high singlet oxygen production rate (relative rate = 1.79). Antitumor photosensitizer-9 exhibits strong phototoxicity against various cancer cells and induces ROS generation under light irradiation. Antitumor photosensitizer-9 inhibits tumor growth in vivo and exhibits excellent anticancer photodynamic therapy (PDT) efficacy at low drug and light doses. Antitumor photosensitizer-9 can be used in photodynamic therapy research.
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DC78685 BMS-181101 hydrochloride
BMS-181101 (hydrochloride) is an orally active antidepressant. BMS-181101 (hydrochloride) can interact with a variety of central presynaptic and postsynaptic 5-HT receptors. BMS-181101 (hydrochloride) can be used in the research of diseases such as depression.
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DC78684 Fluorolintane
Fluorolintane exhibits high affinity for N-methyl-D-aspartate (NMDA) receptors with a Ki of 87.92 nM. Fluorolintane inhibits prepulse inhibition in rats. Fluorolintane also inhibits NMDA receptor-induced field excitatory postsynaptic potentials in rat hippocampal slices.
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DC78683 KDX1381
KDX1381 is a bivalent CK2α inhibitor (IC50: 17 nM, KD: 54 nM). KDX1381 has antitumor activity in mouse 786-O and A375 tumor xenograft models. KDX1381 combined with VEGFR inhibitors or DNA damaging agents enhances antitumor efficacy in mouse hepatocellular carcinoma and glioma models.
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DC78682 E3 ligase Ligand 77
E3 ligase Ligand 77 is a CRBN type E3 ubiquitin ligase ligand. E3 ligase Ligand 77 can be used for synthesizing PROTAC, such as PROTAC RET Degrader 1.
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DC78681 Nebivolol O-β-D-glucuronide
Nebivolol O-β-D-glucuronide is a derivative of Nebivolol. Nebivolol is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease.
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DC78680 Tpl2 Kinase Inhibitor 1 hydrochloride
Tpl2 Kinase Inhibitor 1 hydrochloride is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 hydrochloride plays an important role in the regulation of the inflammatory response and the progression of some cancers.
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DC78679 Nef ligand-1
Nef ligand-1 is the Nef binding part of FC-14367.
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DC78678 QNX-10
QNX-10 is a fatty acid synthase (FASN) inhibitor (IC50 = 0.7 μM) with anticancer activity. QNX-10 exhibits potent FASN inhibition and cytotoxicity against colorectal and breast cancer cells. QNX-10 induces apoptosis and cell cycle arrest in S phase by upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-xL. QNX-10 can be used to investigate anticancer therapies targeting FASN enzymes.
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DC78677 SKF 104351
SKF 104351 is an orally active cytokine suppressive anti-inflammatory drug. SKF 104351 can inhibit TNF-α production.
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DC78676 CSBP ligand 1
CSBP ligand 1 (Compound 36) is a ligand of CSBP, with an IC50 of 0.08 μM for CSBP binding. CSBP ligand 1 can inhibit the production of TNF in mice treated with LPS. CSBP ligand 1 has no significant inhibitory activity against PGHS-1 (IC50: 16 μM) and 5-LO (IC50: 60 μM). CSBP ligand 1 can be used in the research of inflammation-related diseases.
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DC78675 3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid
3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid is a target protein ligand-linker conjugate that incorporates a ligand for c-Met and a PROTAC linker, which recruits E3 ligases. 3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid can be used in the synthesis of PROTACs, such as SJF-8240
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DC78674 CHO-4′Me-5′Br-FUBOXPYRA
CHO-4’Me-5’Br-FUBOXPYRA (CH-FUBBMPDORA) is an oxopyridine carboxamide that shares a similar structure to known synthetic cannabinoids. CHO-4’Me-5’Br-FUBOXPYRA demonstrates limited activation potential at both cannabinoid receptors CB1 and CB2.
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DC78673 L14-8
L14-8 is a potent ferroptosis inducer. L14-8 promotes PLK1 degradation via ubiquitination, increasing TP53 phosphorylation to enhance SAT1 transcription, thereby triggering ferroptosis and cancer cell death. L14-8 can be used for the study of advanced prostate cancer.
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DC78672 KIN-8741
KIN-8741 is a highly selective Type IIb c-Met inhibitor. KIN-8741 has broad activity against c-Met kinase mutations. KIN-8741 shows antitumor activity in MET gene amplified and exon 14 deleted non-small cell lung cancer models. KIN-8741 can be used in the research of c-Met driven cancers, especially advanced tumors carrying MET exon 14 jump mutations, acquired drug resistance mutations, etc.
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DC78671 EGFR ligand-14
EGFR ligand-14 is an EGFR ligand. EGFR ligand-14 can be used for the synthesis of SJF-1521.
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DC78670 Anion transporter-4
Anion transporter-4 (Compound 6) is a small-molecule anion transporter, which induces tubulin degradation and mitochondrial dysfunction. Anion transporter-4 can increase intracellular anion levels such as chloride ions by disrupting microtubule dynamics, promoting lipid peroxidation, and impairing mitochondrial function. Anion transporter-4 triggers ferroptosis to exert anticancer activity. Anion transporter-4 is promising for research of cancers.
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DC78669 JNK-9L
JNK-9L (Compound 9l) is a BBB-penetrable and ATP-competitive JNK inhibitor with IC50s of 0.099 and 0.148  μM for JNK1 and JNK3, respectively. JNK-9L significantly inhibits c-jun phosphorylation and Streptozotocin-induced ROS generation with an IC50 of 0.8  nM. JNK-9L can be used for neurodegenerative disorders like Parkinson’s disease research.
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DC78668 OX2-2303
OX2-2303 is a potent, selective orexin-2 receptor (OX2R) antagonist. OX2-2303 exhibits excellent binding affinity towards OX2R (Ki = 0.1 nM), and shows >890-fold selectivity over OX1R. OX2-2303 can be used as a positron emission tomography (PET) radioligand for central nervous system (CNS) research.
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DC78667 ZN-c5
ZN-c5 is a selective and orally active estrogen receptor degrader. ZN-c5 exhibits high potency in the cellular assay (MCF-7, IC50 = 0.3 nM) and binds with high affinity to ERα and ERβ (IC50 = 0.4 nM and 0.8 nM, respectively). ZN-c5 inhibits tumor growth in MCF-7 mouse xenograft model and WHIM20 xenograft model. ZN-c5 can be used for the study of breast cancer.
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DC78666 ELQ-121
ELQ-121 is a potent inhibitor of the ubiquinol-oxidation (QO)-site of parasites. ELQ-121 has IC50 of 0.05 nM against chloroquine sensitive and multidrug resistant P. falciparum in vitro. ELQ-121 inhibits T. gondii and N. caninum with IC50 below 1 nM in vitro. ELQ-121 suppresses B. besnoiti tachyzoite proliferation with an IC50 of 0.49 nM and induces mitochondrial disruption. ELQ-121 can form polyethylene glycol carbonate ester prodrug which demonstrates in vivo efficacy against P. yoelii in mice. ELQ-121 is suitable for antimalarial research.
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DC78665 ELQ-453
ELQ-453 is an inhibitor targeting the Qo site of the Plasmodium falciparum cytochrome bc1 complex (CytB) with an IC50 value of 0.57 nM. ELQ-453 blocks the mitochondrial function of the parasite, and suppresses Plasmodium infection in mosquitoes. ELQ-453 is promising for research of malaria.
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