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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC79550 MeThPmR
MeThPmR, a ribonucleoside derivative, is a potent and selective human nucleoside transporter 1 (hCNT1) inhibitor (Ki/sub> = 0.16-0.69 μM). MeThPmR exhibit weak inhibitory activity on hCNT2 (IC50 = 360 μM) and hCNT3 (Ki = 4.7 μM). MeThPmR can protect cells from the toxicity of nucleoside drugs. MeThPmR can be used for the research of cancer.
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DC79549 Boc-piperidine-oxopiperidin
Boc-piperidine-oxopiperidin is a PROTAC linker. Boc-piperidine-oxopiperidin can be used to synthesize PROTAC LYA914.
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DC79548 MA203
MA203 is a highly efficient and selective PROTAC degrader targeting CHK1. MA203 accelerates CRBN-dependent proteasomal degradation of CHK1 in solid tumor-derived cells and acute leukemia cells. MA203 induces DNA replication stress. MA203 blocks cell cycle progression and triggers tumor cell apoptosis. MA203 does not damage healthy differentiated and primitive hematopoietic cells, stromal cells, and retinal epithelial cells. MA203 can be used for the study of CHK1-dependent cancers.
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DC79547 (S,S)-PLX-4545
(S,S)-PLX-4545 (Compound I) is an orally active and cereblon-based molecular glue degrader of IKZF2 (zinc finger transcription factor Helios). (S,S)-PLX-4545 can be used for the study of IKZF2-mediated diseases or disorders, such as proliferative diseases or disorders and/or cancer.
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DC79546 ABT-002
ABT-002 is a molecular glue degrader targeting GSPT1 and NEK7. ABT-002 is the active metabolite of ABS-752. ABT-002 is promising for research of hepatocellular carcinoma (HCC).
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DC79545 MI-2-80
MI-2-80 is a molecular glue degrader. MI-2-80 induces proteins (such as IKZF1/3 and CSNK1A1) to bind to CRBN, promoting their ubiquitination and degradation.
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DC79544 L-702958 hydrochloride
L-702958 (hydrochloride) is a potent hERG blocker (IC50 = 14.3 nM). L-702958 (hydrochloride) can be used for research on arrhythmia.
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DC79543 NARS-3′
NARS-3′ is an orally active reversible xanthine oxidase (XO) inhibitor with the IC50 of 21.01 μM. NARS-3′ can competitively inhibit XO activity and reduce uric acid production. NARS-3′ can reduce renal damage in hyperuricemia mice. NARS-3′ can be used for the study of hyperuricemia.
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DC79542 UK-371800
UK-371800 is a highly selective PDE5 inhibitor (IC50 = 4.2 nM). UK-371800 has good permeability and is not affected by the efflux of P-glycoprotein.
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DC79541 CGS-17867A hydrochloride
CGS-17867A (hydrochloride) is a benzodiazepine receptor ligand. CGS-17867A (hydrochloride) has a weak sedative effect and can increase palatable food intake.
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DC79540 F0840-0093
F0840-0093 is a highly selective estrogen receptor α (ERα) degrader. F0840-0093 exhibits potent antiproliferative activity against T47D cells with an IC50 value of 4.65 μM. F0840-0093 is promising for research of estrogen receptor-positive (ER+) breast cancer.
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DC79539 R24
R24 is a type of flavonoid derivative. R24 exhibits strong anti-angiogenic and anti-proliferative effects. R24 induces cell apoptosis and promotes the production of reactive oxygen species (ROS). R24 can be used for the study of cancers such as lung cancer and colorectal cancer.
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DC79538 Morindone
Morindone is an anthraquinone found in Morinda citrifolia L. Morindone can inhibit cancer cells proliferation, induce apoptosis and cause G1 phase arrest. Morindone can inhibit activities of DNA polymerase and downregulate mutated TP53 and KRAS gene expression. Morindone can be used for the research of cancer, such as colon cancer.
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DC79537 SG3683
SG3683 is a DNA-targeted cytotoxic agent belonging to pyrrolobenzodiazepine (PBD) dimers. SG3683 exerts antitumor activity with an IC50 value of 0.74 nM in MDA-MB-436 cells. SG3683 is promising for research of cancers, such as breast cancer.
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DC79536 DV-7751A
DV-7751A is a new Fluoroquinolone and antibacterial agent. DV-7751A inhibits the supercoiling activity of DNA gyrases. DV-7751A exhibits antimicrobial activity against Streptococcus pneumonae, Streptococcus pyogenes, and Peptostreptococcus spp. DV-7751A has a rapid bactericidal effect against S. aureus, Escherichia coli, and P. aeruginosa.
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DC79535 YCJ-02
YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC).
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DC79534 NISC-6
NISC-6 is a novel dual Topo-IIα/Akt inhibitor. NISC-6 has inhibitory activity against various cells, such as UACC903 (IC50 = 2.5 µM) and CHL-1 (IC50 = 0.8 µM) cells. NISC-6 dose dependently induces early and late apoptosis. NISC-6 can be used for research on melanoma.
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DC79533 3'-Ethoxy spinosyn L 17-pseudoaglycone
3'-Ethoxy Spinosyn L 17-pseudoaglycone is an acid degradation product of 3'-ethoxy-5,6-dihydrospinosyn L, a component of the insecticide spinosyn L.
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DC79532 BTF-DNBS
BTF-DNBS is a glutathione (GSH)-responsive small-molecule photosensitizer (PS). BTF-DNBS disrupts mitochondrial function and triggers Golgi-mediated pyroptosis, serving as a reactive oxygen species (ROS) generator. BTF-DNBS is promising for research of cancers.
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DC79531 Y-05460M-A
Y-05460M-A is a substituted isocoumarin antibiotic. Y-05460M-A exhibits inhibitory activity against Gram-positive and Gram-negative bacteria. Y-05460M-A is cytotoxic against P388 lymphatic leukemia. Y-05460M-A also has antiulcer activity. Y-05460M-A is a one-carbon lower homologue of PM-04128. Y-05460M-A can be achieved from N-Boc-L-valine.
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DC79530 GW856464
GW856464 is an antagonist for MCHR1. GW856464 can be studied in research for cardiovascular diseases and obesity.
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DC79529 DS 4574
DS 4574 is an orally active peptidoleukotriene receptor antagonist and mast cell stabilizer. DS 4574 has antiulcer, gastroprotective and antisecretory effects. DS 4574 inhibits various types of experimental asthma models. DS 4574 protects rats from endotoxin-induced intestinal injury.
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DC79528 RLX hydrochloride
RLX (PD 139530) hydrochloride is the hydrochloride of RLX). RLX is a PI3K/Akt/FoxO3a signaling inhibitor, possessing significant therapeutic potential in experimental colon cancer. RLX can effectively modulate the tumor microenvironment, enhancing the efficacy of cancer immunotherapy. RLX demonstrates the ability to improve the retention time of therapeutic agents within the tumor microenvironment by utilizing advanced nanoparticle delivery systems. RLX can be integrated with various treatment modalities, such as chemotherapy and radiotherapy, to enhance overall tumor therapy effectiveness.
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DC79527 TNP-β-L-GTP tetrasodium
TNP-β-L-GTP (TNP-β-L-Guanosine 5'-triphosphate) tetrasodium is a fluorescent GTP mimetic that can be used to study the binding kinetics and affinity of GTP-binding proteins (such as G proteins and GTPases). TNP-β-L-GTP tetrasodium carries a TNP fluorophore, which changes fluorescence intensity upon protein binding, allowing for quantitative analysis.
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DC79526 P-8977
P-8977 is a potent dual CO/5-LO inhibitor (IC50 = 0.01 µM). P-8977 can also inhibit cyclooxygenase (CO) (IC50 = 0.53 µM) in 3T3 cells. P-8977 can inhibit ear edema. P-8977 can be used for research on inflammatory skin conditions.
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DC79525 ML229
ML229 is an HSP90 inhibitor. ML229 can be used in the research of infectious diseases such as candidiasis.
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DC79524 KF-17625
KF-17625 is an orally active bronchodilator. KF-17625 can inhibit bronchoconstriction induced by Carbachol, Histamine, or Leukotriene D4. KF-17625 can inhibit canine tracheal phosphodiesterase (PDE) IV (IC50 = 12 μM) and Concanavalin-A-induced histamine release from rat mast cells (44% inhibition at 10 mM). KF-17625 can be used for the researches of immunology and inflammation.
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DC79523 Sonvuterkib
Sonvuterkib (WX001) is a potent and orally active extracellular signal-regulated kinases (ERK) inhibitor with IC50 values of 1.4, 0.54 nM for ERK1, ERK2, respectively. Sonvuterkib inhibits cell proliferation. Sonvuterkib shows anticancer activity.
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DC79522 TAF1 ligand 1
TAF1 ligand 1 is a TAF1 ligand. TAF1 ligand 1 can be used as a Ligands for Target Protein for PROTAC synthesis, such as ZS3-046.
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DC79521 ZM484
ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.
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