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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC79322 MC3935
MC3935 is a LSD1 inhibitor with an IC50 of 0.52  μM for LSD1-CoREST enzymatic complex. MC3935 has significant antischistosomal activity against transformed schistosomula (NTS) and Schistosoma mansoni adult worms while showing a delayed onset of action towards juvenile forms. MC3935 has no significant toxicity to human cells. MC3935 can be used for schistosomiasis research.
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DC79321 GR 55562
GR 55562 is a selective 5-HT1B receptor antagonist. GR 55562 can be used for the research of nerve disease.
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DC79320 WYE-103914
WYE-103914 is an orally active α7 nAChR (EC50 = 0.49 µM for rat α7 nAChR, EC50 = 0.57 µM for human α7 nAChR) agonist. WYE-103914 exhibits the ability to enhance memory in multiple cognitive models. WYE-103914 is used in combination with antipsychotic drugs. WYE-103914 can be used for research on schizophrenia.
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DC79319 ZnPc-O3-JQ1
ZnPc-O3-JQ1 is a light-triggered BRD4 degrader. Under illumination, ZnPc-O3-JQ1 generates reactive oxygen species (ROS) that degrades BRD4. The degradation of BRD4 results in downregulation of HIF-1α, thereby counteracting the photodynamic therapy (PDT) resistance induced by tumor hypoxia. ZnPc-O3-JQ1 exhibits both Type I and Type II PDT mechanisms.
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DC79318 ZnPc-amide-PEG3-C2-NH2
ZnPc-amide-PEG3-C2-NH2 is a photosensitizer-linker conjugate which consists of ZnPcPs and a linker. ZnPc-amide-PEG3-C2-NH2 can be used to synthesize the photo-activated BRD4 degrader pZnPc-O3-JQ1
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DC79317 TFCA
TFCA is a liver X receptor α (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver.
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DC79316 MMV665917
MMV665917 is an orally active piperazine derivative with anti-Cryptosporidium parvum activity with an EC90 of 15 μM. MMV665917 significantly reduces the parasite load in a porcine model infected with C. hominis, decreases ovarian excretion, alleviates diarrhea symptoms and reduces intestinal mucosal damage. MMV665917 can be used for research on Cryptosporidium parvum disease.
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DC79315 DDP-38003
DDP-38003 (Compound 15) is an orally active KDM1A/LSD1 inhibitor with an IC50 value of 84 nM. DDP-38003 exhibits anticancer activity against promyelocytic leukemia.
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DC79314 WJM664
WJM664 is a potent Plasmodium falciparum PfATP4 inhibitor. WJM664 shows strong activity against malaria parasites. WJM664 blocks gamete development and transmission to mosquitoes by inhibiting PfATP4-mediated Na+-dependent ATPase activity, and acts on multiple stages of the malaria parasite life cycle.
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DC79313 KR-26556
KR-26556 is a sulfonamide type hepatitis B virus (HBV) capsid assembly regulator. KR-26556 exhibits anti-HBV activity with an EC50 of 0.04 μM. KR-26556 has favorable safety characteristics. KR-26556 can be used for research on chronic hepatitis B.
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DC79312 LO-3-62
LO-3-62 is a PROTAC-like SMARCA2/4 degrader with a truncated fumaramide handle. LO-3-62 degrades SMARCA2/4 in cells.
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DC79311 LO-3-61
LO-3-61, a JQ-1 analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.
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DC79310 RN341
RN341 is a specific type II kinase inhibitor of LRRK2 (IC50: 296 nM). RN341 inhibits LRRK2 phosphorylation and avoids S935 dephosphorylation by stabilizing the open conformation. RN341 rescues LRRK2-mediated kinesin motility block by preventing microtubule binding. RN341 effectively inhibits LRRK2 wild-type and G2019S mutant at the cellular level. RN341 provides a new direction for Parkinson's disease research.
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DC79309 FR-182980
FR-182980 is an orally active ACAT1 inhibitor (IC50: 30 nM). FR-182980 has hypocholesterolemic activity and can be used for research of atherosclerosis.
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DC79308 ZWZH-21
ZWZH-21 is a selective and orally active HDAC1/2 dual inhibitor with IC50 values of 34 nM for HDAC1 and 41 nM for HDAC2. ZWZH-21 can inhibit HCT116 and SW480 cells growth with IC50 values of 0.524 μM and 1.063 μM, respectively. ZWZH-21 can inhibit proliferation and migration and induces apoptosis in multiple colorectal cancer cells. ZWZH-21 can be used for the research of cancer, such as colorectal cancer.
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DC79307 LAG-3 Hit II
LAG-3 Hit II is a LAG-3 inhibitor with a KD of 4.32  μM. LAG-3 Hit II can be used for cancers like ovarian cancer, colon adenocarcinoma and melanoma research.
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DC79306 CL-283796
CL-283796 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research.
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DC79305 PRMT5 ligand 2
PRMT5 ligand 2 (Compound 38) is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). PRMT5 ligand 2 can be used for synthesis MS115.
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DC79304 MS115
MS115 is a selective PRMT5/MEP50 PROTAC degrader with DC50 values of 17.4 nM and 11.3 nM for PRMT5 and PRMT5 at 24 h in MDAMB468 cells, respectively. MS115 inhibits the proliferation of breast cancer cells.
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DC79303 E-2101
E-2101 is a novel antispastic agent. E-2101 is a competitive CYP2C19 and CYP2D6 inhibitor with Ki values of 15 and 48 μM, respectively. E-2101 is metabolized by Cytochromes P450 to form monohydroxylated (M1 and M2), dihydroxylated (M3), and N-dealkylated metabolites (M4). E-2101 can be used in the research of skeletal muscle spasm.
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DC79302 KY-9
KY-9 is an antibacterial active compound.
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DC79301 (R)-CFMB
(R)-CFMB is the R-enantiomer of CFMB). CFMB is an agonist of FFAR2- and FFAR3-specific with an EC50 value of 0.8 μM target hFFAR2 and 0.2 μM target rFFAR2.
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DC79300 BAS00602705
BAS00602705 is an E-cadherin inhibitor. BAS00602705 exerts its function by blocking the trans-interactions of E-cadherin molecules within junctional complexes, without permanently altering E-cadherin expression levels. BAS00602705 significantly impairs invadopodia formation in pancreatic cancer cells. BAS00602705 can be used for the study of anti-invasive therapeutic strategies in cancers characterized by dysregulated E-cadherin-mediated invadopodia activity, such as pancreatic ductal adenocarcinoma (PDAC).
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DC79299 (Rac)-Z-FA-FMK
(Rac)-Z-FA-FMK is the racemate of Z-FA-FMK. (Rac)-Z-FA-FMK is an inhibitor of cathepsin B with a Ki of 1.5 μM. (Rac)-Z-FA-FMK inhibits caspase-2, -3, -6, -7, and -9 with IC50s of 6.147, 15.41, 32.45, 9.077, and 110.7 μM. (Rac)-Z-FA-FMK inhibits the main protease of SARS-CoV-2 replication with an IC50 of 11.39 μM. (Rac)-Z-FA-FMK inhibits the increased IL-1β level induced by LPS and NF-κB transactivation in macrophages.
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DC79298 CRBN ligand-185
CRBN ligand-185 is a CRBN ligand. CRBN ligand-185 can be used as a target protein ligand for the synthesis of PROTACs targeting CRBN (Ligands for Target Protein for PROTAC), such as NX-5948.
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DC79297 TBIA
TBIA (trans bis-isatoic anhydride) is a covalent RNA crosslinker. TBIA selectively induces RNA tertiary interactions (e.g., multi-helix junctions, loop-helix packing). TBIA is promising for research of RNA higher-order structure and disease-associated RNAs (e.g., KRAS-mutant RNAs).
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DC79296 (S)-MDL-101146
(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis.
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DC79295 Ciprokiren
Ciprokiren (Ro 44-9375) is a Renin inhibitor with IC50s of 0.07 and 0.65 nM for hRenin in buffer and plasma, respectively. Ciprokiren be applied transdermally with similar hemodynamic effects without decrease of plasma renin activity or plasma immunoreactive angiotensin II. Ciprokiren has antihypertensive efficacy and can be used for hypertension research.
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DC79294 Piperazine-CO-C1-Azacyclohexane-C1-Piperazine
Piperazine-CO-C1-Azacyclohexane-C1-Piperazine is a PROTAC linker can be used in the synthesis of PROTACs, such as PROTAC CDK4/6/9 degrader 1.
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DC79293 SGB-1534 hydrochloride
SGB-1534 (hydrochloride) is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 (hydrochloride) can inhibit vasoconstriction and lower blood pressure. SGB-1534 (hydrochloride) can be used for the research of cardiovascular disease, such as hypertension.
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