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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC79215 E913
E913 is a CCR5 antagonist that competes with the binding of antibodies to CCR5 which recognize the C-terminal half of the second extracellular loop (ECL2B) of CCR5. E913 can specifically block the binding of macrophage inflammatory protein-1alpha (MIP-1alpha) to CCR5 (IC50 = 0.002 μM) and MIP-1alpha-elicited cellular Ca2+ mobilization (IC50 = 0.02 μM). E913 inhibits the replication of laboratory and primary R5 HIV-1 strains as well as various multidrug-resistant monocyte/macrophage tropic (R5) HIV-1 (IC50 = 0.03-0.06 μM). E913 can be used for the research of infection, such as HIV-1 infection.
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DC79213 FE100726
FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research.
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DC79212 ARN25657
ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders.
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DC79211 Aurora kinase inhibitor-14
Aurora kinase inhibitor-14 (Compound 79) is an orally active and highly selective inhibitor of Aurora kinases with IC50 values of 0.5 nM and 1.2 nM for Aurora A and Aurora B, respectively. Aurora kinase inhibitor-14 binds to the ATP-binding site of Aurora kinases to block chromosome segregation during mitosis and induce apoptosis in tumor cells. Aurora kinase inhibitor-14 is promising for research of various solid tumors and hematological malignancies, such as non-small cell lung cancer, breast cancer, and acute myeloid leukemia.
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DC79210 MNFA
MNFA is a derivative of Monofluoroacetic acid. MNFA is an effective pesticide.
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DC79209 KD-027
KD-027 (SLx-2101) is a Phosphodiesterase 5 (PDE5) inhibitor. KD-027 can be used for endothelial dysfunction, and hypertension research.
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DC79208 AHN 070
AHN 070 is an irreversible peripheral benzodiazepine receptor (PBR) ligand. AHN 070 can bind to PBR with nanomolar affinity and is pH-dependent. AHN 070 can be used for studying the structure and function of PBR.
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DC79207 MK-8389
MK-8389 is an orally active LMW allosteric FSH receptor agonist. MK-8389 affects thyroid function.
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DC79206 DNK-333
DNK-333 is a potent and balanced dual NK1 and NK2 receptor antagonist with IC50 values of 4.8 nM and 5.5 nM, respectively. DNK-333 blocks the Neurokinin A (NKA)-induced bronchoconstriction in asthma.
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DC79205 TKA-731
TKA-731 is an NK1 receptor antagonist. TKA-731 can reverse mechanical hyperalgesia. TKA-731 can be used for research on neuropathic pain.
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DC79204 FKBP12 ligand-3
FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels.
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DC79203 EGFR ligand-14-PEG3-Boc
EGFR ligand-14-PEG3-Boc contains EGFR ligand and linker. EGFR ligand-14-PEG3-Boc can be used for the synthesis of SJF-1521.
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DC79202 4-DTM-phenoxy-PEG3-CH2COOH
4-DTM-phenoxy-PEG4-CH2COOH (Formula 3) is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).
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DC79201 Di(4-morpholine-amide)-4-DTM-phenoxy(3,5-F)-O-PEG3-CH2COOH
Di(4-morpholine-amide)-4-DTM-phenoxy(3,5-F)-PEG4-CH2COOH (compound BL) is a cleavable PEG-based ADC linker that can be used in the synthesis of antibody-drug conjugates (ADCs).
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DC79199 TBK1 ligand 2-C-O-C4-O-C3-O-C-amide
TBK1 ligand 2-C-O-C4-O-C3-O-C-amide is a conjugate of TBK1 ligand and linker, which can be used in the synthesis of PROTAC TBK1 degrader-2.
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DC79198 PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu
PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is an Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 and a PROTAC linker. PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu can be used for synthesis of PROTAC BRD4 Degrader-14.
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DC79196 Desisopropyle-belumosudil
KD025m1 is a novel selective ROCK2 inhibitor. KD025m1 has good anti obesity, improved insulin sensitivity, and blood glucose control effects. KD025m1 can be used to study metabolic diseases such as diabetes and obesity.
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DC79192 PD 172760
PD 172760 is a selective D4 receptor antagonist. PD 172760 along with the action of other neurotransmitter receptors may be important in treating psychosis.
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DC79190 DD-04-038
DD-04-038 is a molecular glue degrader. DD-04-038 induces proteins (such as IKZF1/3, ZBED3 and PATZ1) to bind to CRBN, promoting their ubiquitination and degradation.
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DC79189 ALK ligand-Linker Conjugate 1
ALK ligand-Linker Conjugate 1 is a ALK ligand-linker conjugate that can be used for synthesis of PROTAC ALK degrader-4.
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DC79188 NSC 850745
NSC 850745 is a selective and potent c-Met/STAT3 inhibitor with IC50 values of 210 and 670 nM. NSC 850745 can inhibit cell proliferation, induce G2/M phase arrest and induce apoptosis. NSC 850745 can downregulate AKT-1, VEGF and Bcl-2 expression and upregulate p53, Bax and caspase expression. NSC 850745 can be used for the research of cancer, such as leukemia and colon cancer.
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DC79187 SMARCA2/4 Ligand-Linker Conjugate 2
SMARCA2/4 Ligand-Linker Conjugate 2 is a target protein ligand-linker conjugate that can be used to synthesize PROTAC AU-15330.
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DC79186 A2073
A2073 is a flavagline derivative that potently inhibits the proliferation of erythroleukemia cells by causing cell cycle arrest and suppressing the MAPK, NF-κB, and PI3K signaling pathways. A2073 formes stable interactions with cell cycle-related proteins (CDK1, CCNA2, PRIM1). A2073 exhibits significant anti-proliferative activity against tumor cells while maintaining a favorable toxicity profile in a zebrafish xenograft tumor model. A2073 can be used for the study of acute erythroleukemia.
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DC79185 AD-5467
AD-5467 is a potent and selective aldose reductase inhibitor. AD-5467 exhibits antidiabetic effect. AD-5467 can be used for the research of metabolic disease, such as diabetes.
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DC79184 Osunprotafib hydrochloride
Osunprotafib (ABBV-CLS-484) hydrochloride is an orally active and selective active site PTPN1 (IC50: 2.5 nM) and PTPN2(IC50: 1.8 nM) inhibitor. Osunprotafib hydrochloride has 6-8-fold weaker activity on PTPN9 and no detectable activity on SHP-1 or SHP-2. Osunprotafib hydrochloride increases the sensitivity of human cancer cell lines to IFNγ. Osunprotafib hydrochloride generates robust anti-tumor immunity by enhancing JAK-STAT signalling and reducing T cell dysfunction.
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DC79183 CCC-0975
CCC-0975 is a hepatitis B virus (HBV) inhibitor (EC50=10 μM). CCC-0975 interferes with the conversion of relaxed circular DNA (rcDNA) to cccDNA, synchronously reducing cccDNA and its precursor deproteinized rcDNA (DP-rcDNA) without promoting their intracellular degradation. CCC-0975 is promising for research of chronic hepatitis B.
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DC79182 PNU-142586
PNU-142586 is the major metabolite of Linezolid. PNU-142586 can inhibit the activity of DNA topoisomerase 2-α (TOP2A) and DNA topoisomerase 2-β (TOP2B). PNU-142586 interferes with DNA replication and transcription by blocking the binding of DNA to TOP2 and inhibiting ATP hydrolysis. PNU-142586 can be used to study Linezolid-induced hematotoxicity and its molecular mechanism.
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DC79181 FAPI-JNU
FAPI-JNU is a molecule targeting fibroblast activation protein (FAP). FAPI-JNU specifically binds to FAP highly expressed in the tumor microenvironment, and uses radionuclides [68Ga]Ga or [177Lu]Lu to achieve tumor imaging diagnosis. [177Lu]Lu−FAPI−JNU can effectively target and inhibit tumor growth in tumor-bearing mice. FAPI-JNU is promising for research of FAP-positive tumors (such as various solid tumors).
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DC79180 Dacemazine
Dacemazine (Ahistan) is a phenothiazine derivative that acts as a histamine H1 receptor antagonist. Dacemazine exhibits local anesthetic activity and can alleviate spasms induced by acetylcholine and histamine.
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DC79177 PXR ligand-Linker Conjugate 1
PXR ligand-Linker Conjugate 1 is a conjugate of PXR ligand and linker, which can be used to synthesize PROTAC MI1013.
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