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PROTACs

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Cat. No. Product Name Field of Application Chemical Structure
DC81633 Thalidomide-4-O-C9-Br
Thalidomide-4-O-C9-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and a linker used in PROTAC technology. Thalidomide-4-O-C9-Br can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-19.
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DC81632 Thalidomide-4-O-C11-Br
Thalidomide-4-O-C11-Br is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based CRBN ligand and a linker used in PROTAC technology. Thalidomide-4-O-C11-Br can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-23.
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DC81629 TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT
TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT is a drug-linker conjugate for ADC. TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT consists of a topoisomerase 1 inhibitor (Topi MF-6) and a cleavable linker (Maleimide-Ph(3,5-F)-PEG4-Val-Ala). TGA-Val-Ala-NH2-bicyclo[1.1.1]pentane-7-MAD-MDCPT can be used for synthesis of ADCs.
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DC81628 Tezampanel hydrate
Tezampanel (LY293558) hydrate is a potent, selective and competitive NMDA receptor antagonist. Tezampanel hydrate produces postoperative analgesia in rats. Tezampanel hydrate can be used for neuropathic pain research.
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DC81627 tert-Butyl N-methyl-N-(piperidin-4-ylmethyl)carbamate
tert-Butyl N-methyl-N-(piperidin-4-ylmethyl)carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81626 tert-Butyl N-(2-azaspiro[3.3]heptan-6-yl)carbamate hydrochloride
tert-Butyl N-(2-azaspiro[3.3]heptan-6-yl)carbamate hydrochloride is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81625 tert-Butyl 6-amino-2-azaspiro[3.3]heptane-2-carboxylate
tert-Butyl 6-amino-2-azaspiro[3.3]heptane-2-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81623 tert-Butyl 4-(azetidin-3-yl)piperazine-1-carboxylate
tert-Butyl 4-(azetidin-3-yl)piperazine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81619 tert-Butyl 3-(piperazin-1-yl)azetidine-1-carboxylate
tert-Butyl 3-(piperazin-1-yl)azetidine-1-carboxylate is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81616 tert-Butyl (3-(methylamino)propyl)carbamate
tert-Butyl (3-(methylamino)propyl)carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81615 tert-Butyl (2-(azetidin-3-yl)ethyl)carbamate
tert-Butyl (2-(azetidin-3-yl)ethyl)carbamate is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81614 Ternidazole
Ternidazole is a 2-methyl-5-nitroimidazole derivative and an antiprotozoal agent. Ternidazole exhibits antiprotozoal properties and is found to be effective against chronic alcoholism.
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DC81605 TEAD-IN-24
TEAD-IN-24 (Example 65) is a TEAD inhibitor. TEAD-IN-24 exhibits anti-cancer activity against non-small cell lung cancer.
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DC81604 TEAD-IN-23
TEAD-IN-23 (Compound 22) is an efficient pan-TEAD inhibitor with an IC50 of 10 nM. TEAD-IN-23 exhibits potent anti-proliferative activity in both NCI-H226 and MSTO-211H. TEAD-IN-23 causes complete tumor regression in the MSTO-211H xenograft tumor model. TEAD-IN-23 can be used for the study of mesothelioma and hepatocellular carcinoma.
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DC81599 Tazolol
Tazolol is a specific β-adrenergic antagonist (IC50: 700 nM for (-) isoproterenol-elicited accumulation of cyclic AMP in rat cortical slices). Tazolol produces a significant and sustained increase in cardiac output and stroke volume. Tazolol can be used in the research of heart failure.
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DC81598 Tau ligand-2
Tau ligand-2 is a tau aggregate ligand with a Ki value of 0.99 nM. Radiolabeled (18F) Tau ligand-2 serves as a PET tracer. Tau ligand-2 is applicable to research related to Alzheimer's disease.
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DC81595 Tagorizine
Tagorizine is a 5-LOX inhibitor. Tagorizine can be used to study cerebral (or peripheral) blood vessel dilation.
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DC81592 TA-0201
TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1.
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DC81589 SYK-1106
SYK-1106 is a potent delta-opioid receptor (DOR) agonist with an EC50 of 89 pM and a Ki of 848 pM. SYK-1106 is selective for μ and κ opioid receptors, with Ki values of 9.54 nM and 2.45 nM, respectively. SYK-1106 induces dose-dependent antidepressant-like effects. SYK-1106 can be used for the research of depression.
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DC81584 Sulofenur
Sulofenur (LY186641) is an orally active anti-tumor agent. Sulofenur induces gene expression through calcium ion-dependent pathways and some protein kinase-independent pathways, and its effect is particularly enhanced in H-ras mutant cells. Sulofenur exhibits significant activity in mouse solid tumor models and human tumor xenograft models.
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DC81580 STING-IN-17
STING-IN-17 (compound 10a) is an orally active STING (human STING IC50 = 29 nM, mouse STING IC50 = 15 nM) inhibitor. STING-IN-17 can inhibit the phosphorylation of STING, TBK1 and IRF3. STING-IN-17 dose dependently inhibits the mRNA expression of IP10, IFNB1 and ISG56. STING-IN-17 can reduce ROS and inhibit the expression of cleaved-PARP/caspase-3. STING-IN-17 can improve kidney function. STING-IN-17 can be used for research on inflammatory conditions such as acute kidney injury.
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DC81577 STING agonist-48
STING agonist-48 is a potent STING agonist that exhibits STING-dependent activity in vitro (EC50 = 4.02 μM). STING agonist-48 prefers to bind with the transmembrane domain (TMD) over the cytosolic cyclic dinucleotide (CDN) domain. STING agonist-48 shows adjuvant efficacy, enhancing IgG and Th1/Th2 cytokine responses in humanized STING mice. STING agonist-48 can be used for the study of inflammation-related diseases.
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DC81575 Stibophen
Stibophen is a potent antiparasitic agent is effective against Litomosoides carinii, Dipetalonema witei, and Brugia pahangi. Stibophen inhibits lactate accumulation and phosphofructokinases (PFK) activity in adult filariids. Stibophen also inhibits Ascaris and Hymenolepis diminuta PFK without inhibiting mammalian liver PFK. Stibophen can be used for the research of schistosomiasis and filariid infections.
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DC81569 STAT3-IN-52
STAT3-IN-52 (Compound 9) is a selective and orally active signal transducer and activator of transcription 3 (STAT3) inhibitor. STAT3-IN-52 binds to the pY705 site of STAT3 (Ki = 440 nM), blocking the phosphorylation and dimerization of STAT3. STAT3-IN-52 shows strong cytotoxicity against various cancer cells, such as breast cancer MDA-MB-231 (IC50 = 0.7 μM), medulloblastoma UW426, pancreatic cancer BKPC3 cells. STAT3-IN-52 can induce cell apoptosis, inhibit the STAT3 nuclear transport and DNA binding activity and downregulate the expression of the STAT3 target gene MMP9. STAT3-IN-52 can be used for research related to STAT3 abnormal activation in cancer.
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DC81561 Soulattrolide
Soulattrolide is a non-nucleoside HIV-1 reverse transcriptase (RT) inhibitor, antinociceptive, anti-inflammatory, sedative, anxiolytic, and antimicrobial agent with oral effectiveness, IC50 values of 0.34 µM for HIV-1 RT, 69.5 µM for E. coli RNase H, and >495 µM for human DNA polymerase β.Soulattrolide inhibits HIV-1 RT’s DNA-dependent and RNA-dependent DNA polymerase activities, E. coli RNase H activity, and Mycobacterium tuberculosis growth.Soulattrolide shows no activity against HIV-2 RT, AMV RT, RNA polymerase, or HIV-1 RTTyr181, and lacks antidepressant activity.Soulattrolide can be used for the research of HIV-1 infection, pain, inflammation, and Mycobacterium tuberculosis infection.
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DC81556 SNX3-IN-1
SNX3-IN-1 is a sorting nexin 3 (SNX3) inhibitor. SNX3-IN-1 reduces SNX3 protein expression and inhibits SNX3-mediated activation of the Wnt/β-catenin signaling pathway. SNX3-IN-1 inhibits the proliferation and migration of pulmonary fibrosis-related cells, and decreases the expression of fibrosis markers α-SMA and COL-1. SNX3-IN-1 can be used in research related to pulmonary fibrosis.
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DC81553 SMU-C409
SMU-C409 is a TLR1/2 agonist with an EC50 of 65 nM in HEK-Blue hTLR2 Cells. SMU-C409 activates the TLR1/2–MyD88–NF-κB pathway, inducing TNF-α/IL-1β secretion and robust immune cell activation for antitumor immunomodulation. SMU-C409 shows low toxicity in virto. SMU-C409 can be used for cancer immunotherapy research.
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DC81551 SMARCA2/4-ligand-7
SMARCA2/4-ligand-7 is a SMARCA2/4 ligand, which can be used for the synthesis of PROTACs, such as PROTAC SMARCA2/4 degrader-41.
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DC81545 SLD1121
SLD1121 is an agonist of the Wnt/β-catenin signaling pathway that enhances Wnt signaling by targeting LRP6 (Kd: 4.52-7.49 nM). SLD1121 interacts with the intracellular domain of LRP6, stabilizes LRP6, promotes its nuclear translocation, and facilitates its binding to β-catenin, TCF4 or LEF1 in the nucleus, thereby inducing the expression of Wnt-regulated genes and stem cell-related genes. SLD1121 induces the transition of hair follicles from telogen to anagen in the mouse hair growth cycle and promotes hair growth in mice. SLD1121 is applicable to hair loss-related research.
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DC81544 SLC6A19-IN-4
SLC6A19-IN-4 is an allosteric-competitive and orally active B0AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouse B0AT1 with IC50 values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B0AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research.
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