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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
2032 Results for "
target ligand
" in MedChemExpress (MCE) Product Catalog:
Products (2032)
2032 Results for "target ligand" in MCE Product Catalog:
36
36 Publications Verification
Synonyms: TTI-101
Target:
Research Areas:
C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia .
35
35 Cited Publications
Target:
Research Areas:
IWP-2 is an inhibitor of Wnt processing and secretion with an IC50 of 27 nM. IWP-2 targets the membrane-bound O-acyltransferase porcupine (Porcn) and thus preventing a crucial Wnt ligand palmitoylation. IWP-2 is also an ATP-competitive CK1δ inhibitor with an IC50 of 40 nM for the gatekeeper mutant M82FCK1δ .
16
16 Cited Publications
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription .
10
10 Cited Publications
Target:
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SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells .
10
10 Cited Publications
Target:
Research Areas:
SC144 hydrochloride is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 hydrochloride binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 hydrochloride shows potent inhibition of gp130 ligand-triggered signaling. SC144 hydrochloride induces apoptosis in human ovarian cancer cells .
9
PK 11195 (RP 52028) is a ligand of translocator protein (TSPO), which targets Leishmania chemotherapy, with IC50s of 14.2 μM, 8.2 μM, 3.5 μM for L. amazonensis, L. major and L. braziliensis, respectively.
6
6 Cited Publications
Cat. No.: HY-P5321
CAS No.: 152051-61-1
6
6 Cited Publications
Synonyms: 17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate
Target:
Research Areas:
Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
4
Category:
3
3 Cited Publications
Cat. No.: HY-P3267
CAS No.: 11096-37-0
3
3 Cited Publications
Synonyms: NX-5948; BTK-IN-24
Research Areas:
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
3
Target:
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3
3 Cited Publications
Cat. No.: HY-P2264
CAS No.: 676657-00-4
Target:
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3
3 Cited Publications
Cat. No.: HY-P9958A
CAS No.: 615258-40-7
Target:
Research Areas:
2
2 Cited Publications
EN4 is a covalent ligand that targets cysteine 171 (C171) of MYC. EN4 is selective for c-MYC over N-MYC and L-MYC. EN4 inhibits MYC transcriptional activity, downregulates MYC targets, and impairs tumorigenesis .
2
2 Cited Publications
Cat. No.: HY-P3108
CAS No.: 1176306-10-7
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2
2 Cited Publications
Research Areas:
HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).
2
2 Cited Publications
Synonyms: DOTATOC; SDZ-SMT 487; SMT 487
Research Areas:
2
2 Cited Publications
Cat. No.: HY-P1848
CAS No.: 395069-86-0
Target:
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2
Target:
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
