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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC79286 JSZ16
JSZ16 is a Succinate dehydrogenase (SDH) inhibitor with an IC50 of 30.3  μM. JSZ16 has potent broad-spectrum fungicidal activity, such as Sclerotinia sclerotiorum, Botrytis cinerea and Colletotrichum fragariae, with an EC50 of 4.4 mg/L for Sclerotinia sclerotiorum. JSZ16 influences the cell membrane permeability of pathogenic fungi. JSZ16 can be used for the development of fungicide.
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DC79285 PAD-PF1
PAD-PF1 is a PAD4 inhibitor (IC50: 15.9 µM). PAD-PF1 binds to an allosteric site of PAD-PF1, which is distinct from substrate and GSK147.
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DC79284 PAD-PF2
PAD-PF2 is a PAD4 inhibitor with a Kd of  2.82 µM. PAD-PF2 inhibits Ionomycin-induced protein citrullination in human isolated neutrophils.
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DC79283 SB-247853
SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.
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DC79282 ESC1002755
ESC1002755 is a 17β-HSD10 inhibitor with an IC50 of 19 nM. ESC1002755 has significant enzyme specificity with non-/uncompetitive inhibition against the cofactor NADH. ESC1002755 shows minimal cytotoxicity towards the HEK293 at 50 μM. ESC1002755 is promising for Alzheimer’s disease and hormone-dependent cancers (such as prostate, bone and colorectal cancer) research.
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DC79281 BTR2038
BTR2038 is a BRD9 degrader. BTR2038 induces targeted degradation of V5-tagged human BRD9. BTR2038 can be used for the study of biological processes and diseases associated with abnormal BRD9 protein function.
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DC79280 Z88418521
Z88418521 is a ligand for the WDR5-MLL1 complex. Z88418521 may help disrupt the interaction of the WDR5-MLL1 complex. Z88418521 can be used in cancer research, especially in leukemia.
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DC79279 RIPK1 ligand-Linker Conjugate-1
RIPK1 ligand-Linker Conjugate-1 is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for RIPK1 and a PROTAC linker, which recruits E3 ligases. RIPK1 ligand-Linker Conjugate-1 can be used for synthesis of PROTAC RIPK1 Degrader-1
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DC79278 CDD-2110
CDD-2210 is a STK33 inhibitor, with a Kd of 0.1 nM and an IC50 of 38 nM. CDD-2210 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 1209 nM for CLK1, 917 nM for CLK2, 544 nM for CLK4, and 746 nM for RET. CDD-2210 can be used for the study of contraception.
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DC79277 CGR-50
CGR-50 is a potent RSV fusion glycoprotein (F protein) inhibitor (EC50 = 32.6 nM against RSV A2 in HEp-2 cells). CGR-50 blocks RSV entry by binding to the F protein and inhibiting membrane fusion. CGR-50 can be used for RSV infection research.
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DC79276 4SC-207
4SC-207 is a potent, orally active microtubule inhibitor. 4SC-207 inhibits microtubule growth to inhibit tumor cell proliferation in vitro and in vivo, and promotes a mitotic delay/arrest, followed by apoptosis or aberrant divisions. 4SC-207 inhibits tumor growth in taxane resistant xenograft mouse models. 4SC-207 can be used for cancer research, such as colon adenocarcinoma and other malignancies.
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DC79275 Rodin-C
Rodin-C is a selective HDAC inhibitor with IC50s of 0.059, 0.18   and 5.39 μM for HDAC1, HDAC2 and HDAC11, respectively, over HDAC3-10. Rodin-C significantly inhibits the HDAC-CoREST complex with low hematological toxicity. Rodin-C can be used for neurologic disorders such as Alzheimer’s disease research.
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DC79274 Rodin-A
Rodin-A is an orally active, brain-penetrant and selective histone deacetylase (HDAC)-co-repressor of repressor element-1 silencing transcription factor (CoREST) complex inhibitor with an IC50 value of 1.80 μM for the CoREST complex, 0.15 μM for HDAC1, and 0.43 μM for HDAC2. Rodin-A increases the acetylation level of histone H3K9, upregulates the expression of neuron-related genes, thereby promoting the increase in dendritic spine density, the colocalization of synaptic proteins (SV2A and PSD95), and the improvement of hippocampal long-term potentiation (LTP), exerting synaptic protection and repair activity. Rodin-A is promising for research of neurodegenerative diseases related to synaptic dysfunction, especially Alzheimer’s disease.
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DC79273 NASA-linker-VH032-PEG3 ligand
NASA-linker-VH032-PEG3 ligand is a ligand that can be used to synthesize PROTACs.
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DC79272 N-Demethylonalespib
N-Demethylonalespib is a ligand for E3 ligase. N-Demethylonalespib can be used for synthesis of DDO3602.
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DC79271 Thalidomide-N-C-piperidine-C7-Br
Thalidomide-N-C-piperidine-C7-Br, an E3 ligase ligand-linker conjugate, incorporates a cereblon (CRBN) ligand for the E3 ubiquitin ligase and a linker. Thalidomide-N-C-piperidine-C7-Br can be used in the synthesis of ZS3-046.
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DC79270 SK2187
SK2187 is a selective AURKA PROTAC degrader with a DC50 of about 10 nM. SK2187 exhibits growth inhibition against NGP cells with an IC50 of 101.5 nM. SK2187 can be used for the study of MYCN-amplified neuroblastoma.
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DC79269 Thalidomide-piperidine-azetidine-Br
Thalidomide-piperidine-azetidine-Br is an E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and linker. Thalidomide-piperidine-azetidine-Br can be used for synthesis of BY13.
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DC79268 DBCO-HS-PEG2-VA-PABC-SG3199
DBCO-HS-PEG2-VA-PABC-SG3199 is a drug-linker conjugate for ADC. DBCO-HS-PEG2-VA-PABC-SG3199 consists of a SG3199) based DNA small channel crosslinker and cleavable linker. DBCO-HS-PEG2-VA-PABC-SG3199 can be used for synthesis of ADCs.
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DC79267 DBCO-PEG9-amine TFA
DBCO-PEG9-amine (TFA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. DBCO-PEG9-amine (TFA) is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
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DC79266 BTK ligand 11-alcohol-PEG6-azido
BTK ligand 11-alcohol-PEG6-azido is a synthesized E3 ligase ligand-linker conjugate that can be used in the synthesis of PROTACs, such as TDP-43 degrader-1.
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DC79265 CDD-2212
CDD-2212 is a STK33 inhibitor, with a Kd of 1.9 nM and an IC50 of 999 nM. CDD-2212 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 3223 nM for CLK1, 1555 nM for CLK2, 5884 nM for CLK4, and 1093 nM for RET. CDD-2212 can be used for the study of contraception.
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DC79264 Fumiporexant
Fumiporexant (Compound Example 93) is an orally active, brain-penetrant and selective Orexin receptor 2 (OX2R) antagonist. Fumiporexant regulates the sleep-wake cycle and emotion-related pathways in the central nervous system. Fumiporexant is promising for research of nervous system diseases such as insomnia and major depressive disorder.
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DC79263 ACP3 ligand 1
ACP3 ligand 1 (compound I11a) is a ligand against Acid Phosphatase 3 (ACP3, ACPP). ACP3 ligand 1 interacts with ACP3 expressed on the surface of tumor cells for in vivo pharmaco-delivery applications.
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DC79262 CDD-2211
CDD-2211 is a STK33 inhibitor, with a Kd of 0.018 nM and an IC50 of 5 nM. CDD-2211 has relatively weak inhibitory effects on off-target kinases, with IC50 values of 115 nM for CLK1, 48 nM for CLK2, 187 nM for CLK4, and 78 nM for RET. CDD-2211 can be used for the study of contraception.
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DC79261 GRL-098-22
GRL-098-22 (Compound 6t) is a potent inhibitor targeting G protein-coupled receptor kinase 5 (GRK5) and GRK6 with IC50 values of 0.6 μM and 0.19 μM, respectively. GRL-098-22 is promising for research of diseases such as heart failure and multiple myeloma.
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DC79260 QPyN16Th
QPyN16Th is an N-palmitoylated cationic thiazolidine antibiotic. QPyN16Th is selectively active against the Gram-positive bavteria E. faecalis, S. aureus and MRSA with an MIC of 1.95 μM over gram-negative bacteria. QPyN16Th can induce membrane permeabilization and depolarization and ROS production in MRSA. QPyN16Th increases the survival of zebrafish model of intramuscular MRSA infection.
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DC79259 Bay-02752
Bay-02752 (Bay o 2752) is a lipid-lowering agent. Bay-02752 inhibits acyl-CoA activity in liver microsomes (IC50 = 0.95 μg/mL). Bay-02752 inhibits intestinal cholesterol absorption in rats. Bay-02752 inhibits gallstone formation in hamsters.
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DC79258 SUAM 1221
SUAM 1221 is a prolyl endopeptidase inhibitor. CS-0777 can be used in the research of Alzheimer diseases.
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DC79257 DBCO-PEG4-VA-PABC-MMAE
DBCO-PEG4-VA-PABC-MMAE is a drug-linker conjugate for ADC. DBCO-PEG4-VA-PABC-MMAE consists of a tubulin inhibitor (MMAE) and a cleavable linker (DBCO-PEG4-VA-PABC). DBCO-PEG4-VA-PABC-MMAE can be used for synthesis of ADC ABBV-400.
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