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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC75860 PHI-101 PHI-101 is an orally active, potent third-generation inhibitor of FLT3 that overcomes resistance to multiple drug-resistant mutations. It has potential for research in relapsed or refractory acute myeloid leukemia (AML).
DC75861 Bromoenol lactone Bromoenol lactone((6E)-Bromoenol lactone) is a selective, irreversible, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of ≈7 μM. It prevents antigen-stimulated exocytosis in mast cells without hindering Ca2+ influx.
DC75862 Elenestinib phosphate Elenestinib phosphate(BLU-263 phosphate) is a potent and orally active inhibitor of tyrosine kinase that exhibits potent inhibition of c-KIT (D816V) mutation. BLU-263 phosphate has the potential for its use in the research of systemic mastocytosis (SM).
DC75863 Envonalkib Envonalkib(TQ-B3139; CT-71; Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. Envonalkib is also used in the research of non-small cell lung cancer.
DC75864 Cu(II)-Elesclomol Cu(II)-Elesclomol, a Cu2+ complex of Elesclomol, is a weak inhibitor of DNA topoisomerase I. It is also highly capable of inducing cuproptosis and apoptosis. It induces DNA double-strand breaks in K562 cells and causes a G1 cell cycle block. Cu(II)-Elesclomol displays anticancer activity.
DC75865 TI17 TI17 is an inhibitor of thyroid hormone receptor-interacting protein Trip13. TI17 efficiently suppresses the proliferation of multiple myeloma (MM) cells and triggers cell cycle arrest and apoptosis. Trip13, an AAA-ATPase involved in double-strand break (DSB) repair, is targeted by TI17, leading to impaired function and heightened DNA damage.
DC75866 (R)-HTS-3 (GLXC-25878) (R)-HTS-3 (GLXC-25878) is a potent, selective, and cell-active inhibitor of lysophosphatidylcholine acyltransferase 3 (LPCAT3) with an IC50 of 0.09 µM, an enzyme critical for synthesizing C20:4-containing phospholipids. It reduces arachidonic acid-d8 incorporation into phospholipids and mitigates RSL3-induced ferroptosis in HT-1080 and 786-O cancer cells.
DC75867 Ifebemtinib Ifebemtinib(IN10018, BI853520) is a highly selective, potent inhibitor of focal adhesion kinase (FAK), with an IC50 of 1 nM for inhibiting FAK autophosphorylation. It also inhibits FER Kinase and FES Kinase with IC50s of 900 nM and 1040 nM, respectively, inhibiting spheroid formation and orthotopic tumor growth in malignant pleural mesothelioma. IN10018 exhibits anti-tumor activity in vitro and in vivo.
DC75868 AZ14133346 AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75869 MI-217 MI-217 is a potent SIRT3 inhibitor. MI-217 induces MDA-MB-231 apoptosis. MI-217 can be used in the study of breast cancer.
DC75870 (S)-Gebr32a (S)-Gebr32a is a potent PDE4 inhibitor with IC50 values of 19.5, 2.1 µM for PDE4 cat; PDE4D3, respectively.
DC75871 ST80 ST80 is an inhibitor for interaction of OTUD4 and CD73. ST80 decreases CD73 protein level, increases CD73 protein turnover, reduces immune evasion of tumor cells, and thus exhibits antitumor efficacy against immunosuppressive triple-negative breast cancer (TNBC).
DC75872 HL435 HL435 is a heterobifunctional molecule that degrades BRD4 by linking to JQ1, with DC50 of 11.9 nM and 21.9 nM, in MDA-MB-231 and MCF-7 cells, respectively. HL435 inhibits the proliferation of MDA-MB-231, MCF-7, 22Rv1 and A549, arrests the cell cycle and induces apoptosis. HL435 exhibits antitumor activity in mouse model.
DC75873 Rugonersen sodium Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch.
DC75874 Tritetracosanoin Tritetracosanoin (Trilignocerin) is a triacylglycerol of the tetracosanoic acid.
DC75875 BMS-185411 BMS-185411 is a selective retinoic acid receptor alpha (RARα) antagonist, with an IC50 value of 140 nM.
DC75876 Amoitone B Amoitone B, a derivative of cystosporone B, is an agonist of NR4A1. Amoitone B has anticancer activity.
DC75877 7(S)-Maresin 1 7(S)-Maresin 1 is an inactive 7(S) exomer of Maresin 1, containing a 7(R) hydroxyl group. It can be used as a negative control. Maresin 1 is a specific regulator of endogenous DHA production in the human body, which can stimulate the production and secretion of intracellular Ca2+.
DC75878 (Rac)-L-659989 (Rac)-L-659989 is the racemate of L-659989. L-659989 s an orally active, extremely potent, selective and competitive platelet activating factor (PAF) receptor antagonist.
DC75879 MRS8028 MRS8028 is an agonist for A3 adenosine receptor (A3AR), which binds hA3AR with Ki of 2.44 nM. MRS8028 is potential for ameliorating ischemia and inflammatory diseases.
DC75880 Lanepitant Lanepitant (LY303870) is a selective neurokinin-1 (NK-1) receptor antagonist. Lanepitant blocks neurogenic inflammation and pain transmission by preventing the binding of substance P to NK-1 receptors on both neuronal and non-neuronal tissues. Lanepitant can be used to study osteoarthritis.
DC75881 O-Arachidonoyl glycidol O-Arachidonoyl glycidol (compound 1) is a 2-arachidonoylglycerol (2-AG) analog. O-Arachidonoyl glycidol inhibits cytosolic 2-oleoylglycerol (2-OG) hydrolysis with an IC50 value of 4.5 µM. O-Arachidonoyl glycidol blocks 2-OG hydrolysis in membrane fractions and anandamide hydrolysis with IC50s of 19, 12 µM, respectively.
DC75882 Icopezil Icopezil is a selective acetylcholinesterase (AchE) inhibitor. Icopezil can be used in Alzheimer's disease research.
DC75883 HVH-2930 HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab sensitive) and JIMT-1 (Trastuzumab resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclin D1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice.
DC75884 SGR-1505 SGR-1505 is an orally active MALT1 allosteric inhibitor. SGR-1505 inhibits MALT1 enzymatic activity and shows anti-proliferative activity in BTK inhibitor (BTKi)-sensitive and BTKi-resistant activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) cell lines. SGR-1505 can be used for research of B-cell lymphomas.
DC75885 GW814408X GW814408X is a kinase chemical genome group (KCGS) compound that inhibits the AURKC kinase involved in cell cycle progression, checkpoint regulation, and cell division. GW814408X exhibits cell line-dependent toxicity, e.g., cytotoxic effects on HeLa cells. GW814408X acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays.
DC75886 GSK248233A GSK248233A is a dual inhibitor of Fluc and VEGFR2 with IC50 of 1.03 μM and 2 nM, respectively. GSK248233A also shows activity against the AGC family. GSK248233A acts as a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential implications for Fluc reporter assays.
DC75887 GW694590A GW694590A (UNC10112731) is a MYC protein stabilizer that increases endogenous MYC protein levels. GW694590A also targets receptor tyrosine kinases, inhibiting DDR2, KIT and PDGFRα by 81% at 1 μM. , 68% and 67%. GW694590A is a protein kinase inhibitor across ATP-dependent and -independent luciferases with potential effects on the Fluc reporter gene.
DC75888 XRD-0394 XRD-0394 is a potent and specific dual inhibitor of ATM and DNA-PKcs with oral activity. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. In addition, XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro.
DC75889 BDW568 BDW568 is a STING agonist that can selectively activate the human STINGA230 allele. BDW568 can be used to activate STINGA230-engineered macrophages in macrophage-based immunotherapy.

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