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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC77814 ZG297
ZG297 is an agonist for Staphylococcus aureus ClpP (SaClpP ) with an EC50 of 0.26 μM. ZG297 degrades SaFtsZ, inhibits the bacterial cell division, thereby exhibiting antistaphylococcal activity, that inhibits S. aureus 8325-4 strains and MRSA strains with MIC of 0.063-256 μg/mL. ZG297 exhibits anti-infectious efficacy in mouse models.
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DC77813 Zeltociclib
Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.
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DC77812 Z-CITCO
Z-CITCO is the cis isomer of CITCO and a selective ligand for the anti-estrogen binding site (AEBS), the binding affinities (Ki) of PBPE hydrochloride and MBPE to AEBS are 8.79 and 17.57 nM, respectively.
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DC77811 Z-3578
Z-3578 is a small-molecule antagonist targeting MrgX2 (Mas-related G protein-coupled receptor X2) with significant anti-pseudoallergic activity and a KD value of 729 nM. Z-3578 effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, suppressing the release of β-hexosaminidase with IC50 values of 4.90 µM and 6.18 µM, respectively. It also markedly reduces the release of histamine and TNF-α, along with intracellular calcium flux. In a murine pseudoallergy model, Z-3578 significantly alleviates paw swelling and dye extravasation and lowers serum histamine levels, indicating potent in vivo anti-allergic effects. Z-3578 holds promise as a lead compound for the treatment of allergic diseases, especially pseudoallergic reactions.
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DC77810 YX0798
YX0798 is a selective and orally active CDK9 inhibitor (Kd: 0.28 nM). YX0798 downregulates the oncoprotein c-MYC and pro-survival protein MCL-1. YX0798 disrupts the cell cycle and results in transcriptomic reprogramming, eventually leading to cell apoptosis. YX0798 has antitumor activity.
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DC77809 YW3-56 hydrochloride
YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer.
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DC77808 YT 6-2-PEG3-C2-NH2
YT 6-2-PEG3-C2-NH2 is the p62/SQSTM1 targeting, autophagy-targeting ligand-linker conjugate of AUTOTAC ATC-324.
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DC77807 YT 6-2 analog-1
YT 6-2 analog-1 (compound 2-3) is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324.
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DC77806 YT 6-2
YT 6-2 is the p62/SQSTM1 targeting, autophagy-targeting ligand (ATL) of AUTOTAC ATC-324. FGT-4, a TLR7 agonist, is a folate receptor β (FR-β) targeting chimeric molecule.
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DC77805 YNT-3708
YNT-3708 is an orexin receptor (OXR) agonist, with EC50 values of 14.6 nM and 277 nm for OX1R and OX2R, respectively.
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DC77804 YL-1-9
YL-1-9 is an inhibitor of the degradation of p53 by MDM2 through strong binding to the key hydrophobic pockets of MDM2. YL-1-9 induces cell cycle arrest and apoptosis in breast cancer cells.
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DC77803 YJZ5118
YJZ5118 is a CDK12/13 inhibitor with IC50 values of 39.5 nM and 26.4 nM against CDK12 and CDK13, respectively. By inducing DNA damage and Apoptosis, YJZ5118 effectively suppresses tumor cell proliferation and exhibits synergistic effects with Akt inhibitors. YJZ5118 can be used for research in the field of cancer.
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DC77802 XZ338
XZ338 is a highly selective degrader targeting BCL-XL. XZ338 does not degrade BCL-2. XZ338 inhibits MOLT-4 cells with a IC50 value of 3.7 nM. XZ338 has anti-proliferative activity. XZ338 can be used for anti-cancer study.
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DC77801 XT17
XT17 is an anthrone compound with broad-spectrum antibacterial activity. It exerts its antibacterial effect by disrupting the cell wall and inhibiting DNA synthesis. XT17 exhibits weak hemolytic activity, low cytotoxicity against mammalian cell lines, and a low frequency of drug resistance. Meanwhile, XT17 shows in vivo efficacy in a mouse corneal infection model induced by Staphylococcus aureus or Pseudomonas aeruginosa. Further docking studies have confirmed that XT17 can form a stable complex with bacterial gyrase. XT17 can be used in the research of the anti - infection field.
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DC77800 Xeruborbactam isoboxil
Xeruborbactam isoboxil is a beta-lactamase inhibitor.
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DC77799 X-17
X-17 is a Vanin-1 Inhibitor with potent anti-inflammatory and antioxidant activities. X-17 repressrs the inflammatory factor expressions and myeloperoxidase activity, elevats the colonic glutathione reserve, and restors the intestinal barrier.
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DC77798 WQQ-345
WQQ-345 is a BCAT1 inhibitor with an IC50 value of 10.8 mM. WQQ-345 can lead to a decrease in α-KG levels, an upregulation of H3K27me3 expression, a reduction in the expression of glycolytic enzymes (PFKP and LDHA), and impaired glycolytic activity in 67R cells. WQQ-345 shows tumor-suppressing activity in a 67R subcutaneous xenograft model.
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DC77797 Win 45164
Win 45164 is an orally active glucocorticoid receptor (Glucocorticoid Receptor) ligand with the activity of inhibiting the pituitary - adrenal axis. It can promote liver glycogen deposition and thymus involution in adrenalectomized male rats. Meanwhile, Win 45164 has anti - inflammatory effects. It can be used in the research of inflammatory and neurological diseases.
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DC77796 WEHI-3773
WEHI-3773 is an inhibitor of the interaction between VDAC2 and BAK or BAX. WEHI-3773 inhibits BAX-mediated Apoptosis by blocking the VDAC2-mediated recruitment of BAX to mitochondria. Conversely, WEHI-3773 promotes BAK-mediated Apoptosis by limiting the inhibitory sequestration of BAK by VDAC2. WEHI-3773 is promising for research in the field of anti-cancer .
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DC77795 VUF11207 TFA
VUF11207 (Compound 29) TFA is a CXCR7 agonist (pKi of 8.1) that induces recruitment of β-arrestin2 (pEC50 of 8.8) and subsequent internalization (pEC50 of 7.9) of CXCR7.
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DC77794 Viomycin sulfate hydrate
Viomycin sulfate hydrate is a potent antibiotic against Mycobacteria. Viomycin sulfate hydrate rapidly inhibits polypeptide chain elongation when added to purified endogenous Escherichia coli polysomes actively engaged in polypeptide synthesis.
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DC77793 VH 101-amide-piperidine-Pip-alkyne
VH 101-amide-piperidine-Pip-alkyne is an E3 Ligase Ligand-Linker Conjugates that can be used to synthesize PROTAC degrader. The linker part of VH 101-amide-piperidine-Pip-alkyne is tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate, and the VHL-type E3 ubiquitinase ligand is VH 101, acid.
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DC77792 Val-Ala-PAB-SN38
Val-Ala-PAB-SN38 is a Drug-Linker Conjugates for ADC, composed of ADC linker Val-Ala-PAB and SN38, which is the active metabolite of the Topoisomerase I inhibitor irinotecan.
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DC77791 UP163
UP163 enhances the activity of ATPase, and activates valosin-containing protein (VCP) with an EC50 of 9.0 μM. UP163 reduces MG-132. Remdesivir is a nucleoside analogue with effective antiviral activity.
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DC77790 UP158
UP158 enhances the activity of ATPase, and activates valosin-containing protein (VCP) with an EC50 of 2.57 μM.
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DC77789 UP12
UP12 enhances the activity of ATPase, and activates valosin-containing protein (VCP) with an EC50 of 1.24 μM.
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DC77788 Unlabeled FXX489
Unlabeled FXX489 (NNS309) is a fibroblast activation protein (FAP)-targeting ligand. Unlabeled FXX489 can be labeled with 68Ga and 177Lu and shows anticancer effects. Unlabeled FXX489 can be used for the study of pancreatic ductal adenocarcinoma (PDAC), non-small cell lung cancer (NSCLC), breast cancer (BC), and colorectal cancer (CRC).
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DC77787 UNC9435
UNC9435 (compound 44) is a dual inhibitor of TYRO3/MERTK with IC50 values of 3.7 nM and 1.1 nM, respectively. UNC9435 reduces colony formation in non-small cell lung cancer cultures
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DC77786 UNC8212
UNC8212 is a TAM kinase inhibitor. UNC8212 has potent inhibitory activity against MERTK and AXL (IC50: 1.5 nM and 1.3 nM, respectively), and also inhibits TYRO3 (IC50: 6.7 nM). UNC8212 mediates polypharmacological properties by targeting the structurally diverse "back pocket" region of the TAM kinase family. UNC8212 binds tightly to TAM kinases and potently inhibits MERTK and AXL phosphorylation. UNC8212 has anti-tumor effects and can be used in cancer immunotherapy and tumor cell targeting research.
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DC77785 UNC6535
UNC6535 is a potent and reversible SETDB1 triple Tudor domain (3TD) ligand, with an IC50 of 3.4 µM. UNC6535 occupies simultaneously both the TD2 and TD3 reader binding sites. UNC6535 weakly inhibits SETDB1 methyltransferase activity, with an IC50 of 84 µM for the full-length protein. UNC6535 lacks selectivity for the 3TD and may also interact with the SET domain.
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