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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC28635 NH-bis-PEG2
NH-bis-PEG2 is a non-cleavable 2 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28633 Br-PEG4-C2-Boc
Br-PEG4-C2-Boc is a cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28632 Amino-PEG11-OH
Amino-PEG11-OH is non-cleavable 11 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28631 Propargyl-PEG4-CH2CH2-Boc
Propargyl-PEG4-CH2CH2-Boc is a PEG- and Alkyl/ether-based non-cleavable ADC linker. Propargyl-PEG5-Boc can used to synthesize ADC inhibitors of Galectin-3.
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DC28630 HIF-2α-IN-2
HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA).
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DC28629 Mal-PEG2-Val-Cit-amido-PAB-OH
Mal-PEG2-Val-Cit-amido-PAB-OH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28628 Azido-PEG5-alcohol
Azido-PEG5-alcohol is a non-cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Azido-PEG5-alcohol is also a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
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DC28627 Azido-PEG5-CH2CO2H
Azido-PEG5-CH2CO2H is a cleavable 5 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28626 Sapienic acid sodium
Sapienic acid sodium is a fatty acid commonly found on the skin and in mucosa. Sapienic acid sodium has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid sodium is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively.
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DC28625 Sapienic acid
Sapienic acid is a fatty acid commonly found on the skin and in mucosa. Sapienic acid has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively.
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DC28622 Propargyl-PEG8-NH2
Propargyl-PEG8-NH2 (compound 3b) is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28621 Fmoc-NH-PEG4-CH2COOH
Fmoc-NH-PEG4-CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28620 Azido-PEG9-amine
Azido-PEG9-amine is a non-cleavable 9 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28619 Fmoc-NH-PEG9-CH2CH2COOH
Fmoc-NH-PEG9-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28618 Amino-PEG9-acid
Amino-PEG9-acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28617 Tr-PEG8-OH
Tr-PEG8-OH is a non-cleavable 8 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
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DC28614 Hypoglycemic agent 1
Hypoglycemic agent 1 acts as a therapeutic and/or prophylactic agent for diabetes. Hypoglycemic agent 1 has an action for lowering blood sugar.
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DC28613 CDK9-IN-9
CDK9-IN-9 (example 2) is a potent and selective CDK9 inhibitor with an IC50 of 1.8 nM. CDK9-IN-9 inhibits CDK2 with an IC50 of 155 nM. CDK9-IN-9 has anti-cancer activity.
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DC28612 Luteolinidin chloride
Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
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DC28611 TSHR antagonist S37
TSHR antagonist S37 is a selective and competitive thyrotropin receptor (TSHR) antagonist. TSHR antagonist S37 is the racemate of TSHR antagonist S37a.
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DC28610 TSHR antagonist S37a
TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
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DC28609 PROTAC IRAK4 degrader-1
PROTAC IRAK4 degrader-1 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.
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DC28608 (S)-BI 665915
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production.
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DC28607 MJ33 lithium
MJ33 lithium is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 lithium blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6. MJ33 lithium has a critical effect on inflammatory brain damage.
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DC28605 Benzothiohydrazide
Benzothiohydrazide is an analogue of anti–tubercular agent Isoniazid. Benzothiohydrazide exhibits anti–tubercular activity, with MICs of 132 μM and 264 μM for M. tuberculosis wild type (H37Rv) and clinical mutant strains (IC1 and IC2).
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DC28604 S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate
S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is a glutathione cleavable ADC linker used for the antibody-drug conjugates (ADCs) and refers to the Alkyl-Chain composition. S-(1-Hydroxy-2-methylpropan-2-yl) methanesulfonothioate is the linker portions of the molecules employed for mAb attachment purposes.
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DC28603 PROTAC BRD4 ligand-1
PROTAC BRD4 ligand-1 is a potent BET inhibitor and a ligand for target BRD4 protein for PROTACT.
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DC28602 GNE-987
GNE-987 is a highly active chimeric BET degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 incorporates a potent BET binder/inhibitor, a VHL-binding fragment, and a ten methylene spacer moiety. GNE-987 can be used in PROTAC-Antibody Conjugate (PAC).
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DC28601 (S)-GNE-987
(S)-GNE-987 (compound 4), the GNE-987 (a chimeric BET degrader) hydroxy-proline epimer, abrogates binding to VHL and does not degrade BRD4 protein. (S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
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DC28600 KB02-JQ1
KB02-JQ1 is a highly selective and PROTAC-based BRD4 degrader (molecular glue), but does not degrade BRD2 or BRD3. KB02-JQ1 promotes BRD4 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. JQ1 binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-JQ1.
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