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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC79695 Idrabiotaparinux sodium
Idrabiotaparinux sodium is a derivative of Idraparinux synthesized with biotin. Idraparinux is a polymethylated synthetic pentasaccharide known to interact with the antithrombin III and act as anticoagulant.
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DC79694 BIIB021 mesylate
BIIB021 (CNF2024) mesylate is the mesylate of BIIB021. BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC50 values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML.
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DC79693 AMG-126737
AMG-126737 is an orally active and highly selective human mast cell tryptase inhibitor with a Ki of 90 nM. AMG-126737 suppresses early/late-phase bronchoconstriction in sheep models. AMG-126737 is promising for research of asthma and allergic diseases.
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DC79692 LMD-902
LMD-902, a LMD-009) analog, is a CCR8 agonist with an EC50 of 15  nM. LMD-902 has a superior binging capacity depending on key residues such as PheVI:16. LMD-902 can be used for inflammation diseases like bronchial asthma and central nervous system diseases like multiple sclerosis research.
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DC79691 Diosuxentan
Diosuxentan is an inhibitor of ETA. Diosuxentan can be used in research for cardiovascular, renal and neuronal inflammation diseases.
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DC79690 ABT-866
ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence.
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DC79689 L 373890
L 373890 is a selective pyridinone acetamide thrombin inhibitor with a Ki of 0.5 nM. L 373890 shows highly selectivity for thrombin over trypsin (Ki of 570 nM), serine proteases plasmin, tPA, activated protein C, plasma kallikrein and chymotrypsin. L 373890 can be used for thrombosis research.
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DC79688 sCNH240
sCNH240 (Compound P1) is an oral active and selective Rv1625c/Cya activator. sCNH240 has significant anti-tuberculosis activity with a MIC90 of 1.24 μM for Mycobacterium tuberculosis (Mtb) H37Rv strain on cholesterol. sCNH240 can be used for tuberculosis treatment research.
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DC79687 BBT-176
BBT-176 is an orally effective EGFR inhibitor. BBT-176 has inhibitory activity against multiple EGFR C797S mutant cell lines. BBT-176 is commonly used in cancer research.
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DC79686 PI3Kα Ligand-1
PI3Kα Ligand-1 is the ligand for PI3Kα that can be used for synthesis of PROTACs, such as PI3Kα degrader-1.
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DC79685 MK 6325
MK 6325 is a HCV NS3/4a protease inhibitor. MK 6325 displays the broad genotype and mutant potency. MK 6325 can be used for the research of infection.
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DC79684 ML 083
ML083 is a member of a series of highly specific allosteric activators for the tumor-specific isoform of human pyruvate kinase (M2 isoform). ML083 affects the cooperativity of phosphoenolpyruvate (PEP) binding. ML083 can be used in the research of tumors.
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DC79683 UK-224671
UK-224671 is a potent and selective NK2 receptor antagonist. UK-224671 is affected by P-gp efflux and poor intrinsic membrane permeability, resulting in low oral bioavailability.
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DC79682 rel-A-395 hydrochloride
rel-A-395 hydrochloride is the relative configuration of A-395) hydrochloride. A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
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DC79681 KZR-261
KZR-261 is a Sec61 inhibitor. KZR-261 directly binds to the Sec61 channel to potently inhibit the biogenesis of a subset of Sec61 client proteins. KZR-261 has a broad antitumor activity (such as colorectal pancreas and prostate cancer), along with the activation of an endoplasmic reticulum stress response, with minimal adverse effects on normal cells. KZR-261 significantly induces apoptosis of H929 cells. KZR-261 potently inhibits tumor growth in multiple xenograft tumor mice models with good tolerance.
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DC79680 (Rac)-IBR120
(Rac)-IBR120 is the racemate of IBR120. IBR120 is a RAD51 inhibitor that has significant growth inhibition activity against MDA-MB-468 cells. (Rac)-IBR120 can be used for the research of difficult-to-treat cancers like triple negative breast cancer.
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DC79679 Tegacorat
Tegacorat (Compound 447) is a glucocorticoid receptor agonist with an EC50 < 100 nM. Tegacorat can be used in the research of inflammatory diseases.
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DC79678 SB 258741
SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.
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DC79677 UR-12947
UR-12947 is a platelet glycoprotein (GP) IIb-IIIa antagonist. UR-12947 exhibits potent inhibitory activity against platelet aggregation in human platelet-rich plasma, with an IC50 value of 3.5 nM. UR-12947 can be used in the research of arterial thrombotic diseases.
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DC79676 Vizenpistat
Vizenpistat is an ENPP1 inhibitor that can be used in the study of cancer.
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DC79675 DPC 684
DPC 684 is a potent and selective HIV-1 protease inhibitor (IC90 = 5.7-40 nM, Ki = 0.021 nM). DPC 684 competitively inhibits HIV-1 protease and blocks viral polyprotein cleavage. DPC 684 has low protein binding and broad-spectrum inhibition against a variety of wild-type and mutant HIV-1 proteases. DPC 684 has low protein binding and broad-spectrum inhibition (IC90 = 1.9-6.3 nM). DPC 684 has research significance for HIV.
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DC79674 CH4933468
CH4933468 is a thiohydantoin derivative, shows androgen receptor (AR) pure antagonist activity in vitro. CH4933468 inhibits AR-mediated transactivation and proliferation of LNCaP and LNCaP-BC2 cells. CH4933468 can be used for castration-resistant prostate cancer (CRPC) research.
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DC79673 Saviprazole
Saviprazole is a Proton Pump inhibitor. Saviprazole can be used in research related to gastrointestinal diseases, such as gastric ulcers and acid reflux.
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DC79672 BAY-1112054 hydrochloride
BAY-1112054 (BAY-958) (hydrochloride) is a potent PTEFb/CDK9 inhibitor with high selectivity demonstrated, particularly within the CDK family. BAY-1112054 (hydrochloride) shows strong antiproliferative activity against cancer cell lines such as HeLa and MOLM-13. BAY-1112054 (hydrochloride) exhibits good metabolic stability. BAY-1112054 (hydrochloride) effectively inhibits tumor growth in mouse xenograft models without significant toxicity.
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DC79671 BMS-187308
BMS-187308 is an orally active endothelin-A (ETA) antagonist, with Kis of 4.7 nM for ETA and 1.7 μM for ETB. BMS-187308 inhibits the pressor response to ET-1 (ED25: 1.2 µmol/kg; iv). BMS-187308 is a suitable tool for investigating the role of endothelin.
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DC79670 GSI-136
GSI-136 is an inhibitor of γ-secretase with an IC50 of 3 nM. GSI-136 can be studied in medicinal and agricultural chemistry research.
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DC79669 SR-4559
SR-4559 (Compound 4) is a α/β hydrolase domain-containing protein 5 (ABHD5) ligand. SR-4559 activates adipose triglyceride lipase (ATGL) and stimulates lipolysis by inhibiting ABHD5-PLIN interactions in adipocytes and muscle cells. SR-4559 can be used for metabolic diseases like Chanarin Dorfman syndrome research
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DC79668 NU6301
NU6301 is a NU6102 (a CDK2 inhibitor) prodrug. NU6301 can rapidly generate NU6102 in mouse plasma. NU6301 has anticancer activity against endometrial cancer.
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DC79667 TrkA Inhibitor
TrkA Inhibitor (Compound 18) is a CDK2 inhibitor with an IC50 of 0.69  μM over CDK1. TrkA Inhibitor can be used for chemotherapy-induced alopecia research.
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DC79666 GSK4418959 (enantiomer)
GSK4418959 enantiomer is an enantiomer of GSK4418959. GSK4418959 (IDE275) is a non-covalent, reversible, selective and orally active WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer.
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