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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC81672 trans-4-[[(1,1-Dimethylethoxy)carbonyl]amino]cyclohexaneacetic acid
trans-4-[[(1,1-Dimethylethoxy)carbonyl]amino]cyclohexaneacetic acid is a PROTAC linker that can be used in the synthesis of PROTACs.
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DC81671 trans-​2-​Methoxycinnamic acid
trans-2-Methoxycinnamic acid (Compound 6) is a trans-cinnamic acid derivative. trans-2-Methoxycinnamic acid inhibits α-glucosidase with an IC50 of 4.34 mM. trans-2-Methoxycinnamic acid can be used in the research of HIV infection and hyperglycemia.
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DC81670 Tramadol N-oxide
Tramadol N-oxide (RWJ 38705) is an analgesic. Tramadol N-oxide sproduces dose-related, long-lasting antinociception. Tramadol N-oxide has affinity for μ opioid receptor (Ki = 38.5 μM) and δ, κ receptors (Ki > 100 μM). Tramadol N-oxide can be used for the study of analgesic effect.
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DC81669 TPP@CUR
TPP@CUR is the product formed by the esterification reaction between Curcumin and (5-hydroxy-5-oxopentyl)triphenylphosphonium bromide (TPP). TPP@CUR can be used to synthesize Ser@TPP@CUR, which can then be used in studies of acute kidney injury.
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DC81668 TP receptor antagonist-3
TP receptor antagonist-3 (compound 51280) is a potent thromboxane A2 prostanoid (TP) receptor with an IC50 of 15.7 nM against Human TP. TP receptor antagonist-3 can be used for alzheimer's disease, cardiovascular and respiratory diseases, and cancer research.
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DC81667 Topoisomerase ll/ME-1-IN-1
Topoisomerase ll/ME-1-IN-1 (Compound 7a) is a Topoisomerase ll and ME-1 inhibitor with an IC50 of 5.03 μM against Topoisomerase ll. Topoisomerase ll/ME-1-IN-1 functionally inhibits the activity of Topoisomerase II and functionally blocks the activity of ME-1. Topoisomerase ll/ME-1-IN-1 induces Autophagy by upregulating the expression of Beclin-1 and LC3-II. Topoisomerase ll/ME-1-IN-1 promotes Apoptosis. Topoisomerase ll/ME-1-IN-1 exhibits antiproliferative activity against breast cancer cells and shows no toxicity to normal mammary epithelial cells. Topoisomerase ll/ME-1-IN-1 can be used in studies related to breast cancer (including triple-negative breast cancer).
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DC81666 Topoisomerase IV-IN-3
Topoisomerase IV-IN-3 is a Staphylococcus aureus Topoisomerase IV inhibitor, DNA gyrase inhibitor and antibacterial agent. Topoisomerase IV-IN-3 has IC50 values of 1.32 μM and 0.48 μM against topoisomerase IV, and 0.88 μM and 0.54 μM against DNA gyrase. Topoisomerase IV-IN-3 inhibits decatenation, ATPase, and supercoiling activities of its target enzymes. Topoisomerase IV-IN-3 exerts antibacterial activity against Gram-positive and Gram-negative bacterial strains. Topoisomerase IV-IN-3 exhibits low cytotoxicity toward human fibroblast cells. Topoisomerase IV-IN-3 can be used for the research of bacterial infections.
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DC81665 Topoisomerase I-IN-19
Topoisomerase I-IN-19 (Example 36) is a Topoisomerase I inhibitor. Topoisomerase I-IN-19 can be used to investigate Topoisomerase I-mediated diseases such as cancer.
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DC81664 TOP1/TDP1-IN-1
TOP1/TDP1-IN-1 is a DNA topoisomerase 1B (TOP1) and tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with a TDP1 IC50 of 17.8 μM. TOP1/TDP1-IN-1directly suppresses TOP1 catalytic activity without forming a DNA-TOP1 ternary complex, inhibits TDP1-mediated repair of TOP1-induced DNA damage, and exhibits low acute toxicity. TOP1/TDP1-IN-1 disrupts DNA repair pathways, induces apoptosis, suppresses clonogenic growth, and elicits antiproliferative effects in cancer cells. TOP1/TDP1-IN-1 can be used for the research of non-small cell lung cancer, cervical cancer, colon cancer.
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DC81663 Tomoxiprole
Tomoxiprole (MDL 035) is a new analgesic antiinflammatory agent. Tomoxiprole selectively inhibits cyclooxygenase-2 (IC50 = 7 nM) .
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DC81662 TNIK-IN-10
TNIK-IN-10 (Compound N15) is a TNIK inhibitor with an IC50 of 0.49 nM against human TNIK. TNIK-IN-10 inhibits the enzymatic activity of TNIK, downregulates the expression of Wnt pathway target genes c-Myc and AXIN2, and reduces the protein expression of LRP5 and LRP6. TNIK-IN-10 induces apoptosis. TNIK-IN-10 exhibits anticancer activity against colorectal cancer. TNIK-IN-10 can be used in the research of colorectal cancer.
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DC81661 TNIK modulator-1
TNIK modulator-1 (example 12) is a TNIK modulator.
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DC81660 TNF-α-IN-28
TNF-α-IN-28 (compound 4ea) is a TNF-α and NF-κB inhibitor with anti-inflammatory activity. TNF-α-IN-28 inhibits TNF-α and NF-κB expression. TNF-α-IN-28 interacts with TNF-α dimer.
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DC81659 TMLZ-G46
TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research.
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DC81658 TMLB-C16
TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a KD of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC50 = 6.53 μM) and HCCLM3 cells (IC50 = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research.
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DC81657 TMEM175 modulator 3
TMEM175 modulator 3 (Compound 14) is a TMEM175 modulator. TMEM175 modulator 3 can be used in research on neurodegenerative diseases.
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DC81656 TMC-169
TMC-169 is a potent antibiotic of the Aspochalasin group that can be isolated from Aspergillus flavipes. TMC-169 exhibits anti-tumor activity against multiple cancer cells. TMC-169 can be used for the research of cancer, such as hematologic malignancies, non-small cell lung cancer, breast cancer, and glioma.
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DC81655 TLX agonist 3
TLX agonist 3 is a potent and selective tailless homolog (TLX, NR2E1) agonist with an EC50 of 0.25 μM and a Kd of 1.6 μM). TLX agonist 3 shows high selectivity over related nuclear receptors, and promotes TLX oligomerization with an EC50 of 5.0 μM. TLX agonist 3 can be used for the research of neurodegenerative diseases.
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DC81654 TLR9 antagonist 2
TLR9 antagonist 2 is a highly selective and water-soluble TLR9 antagonist with an IC50 of 13 nM against human TLR9. TLR9 antagonist 2 inhibits CpG-induced production of the pro-inflammatory cytokine IL-6. TLR9 antagonist 2 is applicable for research on systemic, TLR9-mediated uncontrolled inflammatory responses, such as sepsis.
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DC81653 TLR8 agonist 10
TLR8 agonist 10 is a selective TLR8 agonist with an EC50 of 0.019 μM in humans. TLR8 agonist 10 activates TLR8-mediated signaling pathways. As a latency-reversing agent, TLR8 agonist 10 reactivates latent HIV-1 reservoirs. TLR8 agonist 10 activates innate cytotoxic natural killer cells to target HIV-infected CD4+ T cells. TLR8 agonist 10 is applicable to research related to HIV-1 infection.
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DC81652 TLR7 antagonist-1
TLR7 antagonist-1 (Compound 44#) is an orally active, selective TLR7 antagonist with an IC50 value of 0.3 nM against TLR7. TLR7 antagonist-1 selectively binds to TLR7, inhibits its activation, and downregulates the c-Rel signaling pathway. TLR7 antagonist-1 downregulates the mRNA levels of proinflammatory cytokines IL-1β, IL-6, and TNF-α. TLR7 antagonist-1 alleviates Imiquimod-induced psoriasis-like skin lesions. TLR7 antagonist-1 is applicable to research related to psoriasis.
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DC81651 TLR7 agonist 33
TLR7 agonist 33 (Compound 141) is a potent TLR7 activator with an EC50 of 1 nM. TLR7 agonist 33 can be used for cancer research.
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DC81650 TLR7 agonist 31
TLR7 agonist 31 (Compound 116) is a TLR7 agonist, with an EC50 of 31 nM. TLR7 agonist 31 can be used in the research of cancer.
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DC81649 TLR2/9 antagonist 1
TLR2/9 antagonist 1 (Compound 24) is a reversible covalent TLR2 (IC₅₀ = 0.5 μM (TLR2/TLR6); IC₅₀ = 0.6 μM (TLR2/TLR1)) and TLR9 (IC₅₀ = 0.32 μM) antagonist. TLR2/9 antagonist 1 has no significant effect on other TLR subtypes. TLR2/9 antagonist 1 can be used for studying central nervous system diseases and malignant tumors caused by inflammation.
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DC81648 TLD-1433
TLD-1433 is the fourth-generation ruthenium (II) based photodynamic compound (PDC). TLD-1433 is activated by green light (525 ± 25 nm) and efficiently generates ROS to achieve pathogen inactivation. After photoinactivation, TLD-1433 significantly induces lipid peroxidation of the cell membrane, which can directly damage the integrity of the viral envelope. TLD-1433 has ID50 for enveloped viruses (such as H1N1 influenza virus, coronavirus OC43, HSV-1, Zika virus) is as low as nanomolar level; for non-enveloped viruses (such as adenovirus Ad5, mammalian rotavirus MRV), a concentration of micro-molar level is required for inactivation. TLD-1433 has antigen retention property and can be used for the preparation of inactivated vaccines.
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DC81647 TKP-5
TKP-5 is a PROTAC protein degrader targeting BRD4. TKP-5 can binds to BRD2, BRD3, BRD4 and BRDT, with Ka values of 150 nM, 100 nM and 150 nM for the first three proteins respectively. TKP-5 inhibits the production of thymic stromal lymphopoietin and suppresses the expression of IL-33 mRNA. TKP-5 is applicable to studies related to tape-stripping induced skin injury. (Pink: Epigenetic Reader Domain ligand ; Blue: Cereblon ligand ; Black: linker).
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DC81646 TKL002
TKL002 is a blood-brain barrier-permeable inhibitor of the CTH/H2S/NF-κB/EMT signaling axis. TKL002 induces G2/M phase cell cycle arrest and apoptosis in glioblastoma cells. TKL002 inhibits the migration and invasion of glioblastoma cells by upregulating E-cadherin and downregulating N-cadherin and vimentin. TKL002 is applicable to relevant research on glioblastoma.
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DC81645 TJN 220
TJN 220 is a synthetic derivative of orally active tetrandrine. TJN 220 has a long-lasting and stable antihypertensive effect in various hypertension models. TJN 220 is suitable for controlling nighttime hypertension and does not cause reflex tachycardia. TJN 220 can be used for research on hypertension.
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DC81644 Tizetatug rezetecan
Tizetatug rezetecan (SHR-A1921) is an Antibody-drug Conjugate (ADC) composed of antibody Tizetatug and MC-Gly-Gly-Phe-Gly-(R)-Cyclopropane-Exatecan. Tizetatug rezetecan can be used for the research of cancer.
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DC81643 TIPARP-IN-1
TIPARP-IN-1 (Compound 15) is a selective PARP7 (TIPARP) (2,3,7,8-Tetrachlorodiben-zo-p-dioxin(TCDD)-inducible PARP) inhibitor with an IC50 of 2.15 nM. TIPARP-IN-1 can restore IFN signaling pathway in tumors by inhibiting TIPARP. TIPARP-IN-1 selectively activates the anti-tumor immune response in the tumor microenvironment and avoids the production of systemic cytokines. TIPARP-IN-1 can be used for research of head and neck squamous cell carcinoma.
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