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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
12 Results for "
hydrophobic channel
" in MedChemExpress (MCE) Product Catalog:
Products (12)
12 Results for "hydrophobic channel" in MCE Product Catalog:
2
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1 Cited Publications
Cat. No.: HY-P2324
CAS No.: 11029-61-1
Cat. No.: HY-120078
CAS No.: 1845753-81-2
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AZD2716 is an orally active secretory phospholipase A2 (sPLA2) inhibitor. AZD2716 inhibits human GIIA sPLA2 (IC50=10 nM), human GV sPLA2 (IC50=40 nM), human GX sPLA2 (IC50=400 nM), snake venom sPLA2 (IC50=2 pM), and snake (Bothrops jararacussu) Lys49-PLA2-like toxin (Kd=110 μM). AZD2716 inhibits sPLA2 isoforms IIa, V, X, snake venom sPLA2s, and snake venom Lys49-PLA2-like toxin myotoxic activity via hydrophobic channel binding. AZD2716 suppresses GIIA sPLA2 production, neutralizes snake venom-induced myotoxicity, and improves survival in envenomed mice. AZD2716 can be used for the research of coronary artery disease, atherosclerosis, and snakebite envenoming .
Cat. No.: HY-126233
CAS No.: 1689554-51-5
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PAT-347 is an inhibitor of autotaxin (ATX, ENPP-2) . PAT-347 binds only to the hydrophobic channel of ATX, without occupying its hydrophobic pocket and catalytic site . PAT-347 blocks the binding of lysophosphatidylcholine (LPC) to the catalytic site of ATX .
Cat. No.: HY-172140
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Ebio3 is a selective potassium channel (KCNQ2) inhibitor with an IC50 of 1.2 nM. Ebio3 binds to the KCNQ2 channel through its hydrophobic tail, causing the S6 helix to move inward, which leads to the closure of the inner gate. The inhibitory effect of Ebio3 is also effective in pathogenic mutants of KCNQ2 (such as R75C and I238L), where it can inhibit outward currents by more than 80%. Ebio3 is expected to be used in the research of neurological diseases such as epilepsy .
Cat. No.: HY-P2324A
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Cat. No.: HY-126230
CAS No.: 1781233-84-8
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PAT-494 is an ATX inhibitor with significant activity in biochemical and plasma assays. PAT-494 can reduce LPA levels in rat plasma through oral administration. The structure-activity relationship study of PAT-494 shows that its binding mode with ATX is novel and it can effectively occupy the hydrophobic pockets and channels of ATX .
Cat. No.: HY-120646
CAS No.: 1675204-51-9
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BMS-242 is a small molecule PD-1/PD-L1 inhibitor with the activity of inhibiting the PD-1/PD-L1 interaction. BMS-242 can bind to the hydrophobic channel pocket between PD-L1 molecules, inhibit the PD-1/PD-L1 immune checkpoint pathway, and provide a new way for cancer inhibition.
Cat. No.: HY-126229
CAS No.: 1682644-84-3
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PAT-078 is a type II autotaxin (ATX) inhibitor. PAT-078 mainly occupies the hydrophobic pocket of ATX, blocks the bottleneck region between the hydrophobic channel and the catalytic site, and does not interact with the zinc ion at the catalytic site .
Cat. No.: HY-181128
CAS No.: 2253948-15-9
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QO-83, Retigabine analogue, is a voltage-gated potassium channel KCNQ2 (Kv7.2) activator with an EC50 of 0.56 μM. QO-83 binds to a single hydrophobic pocket of KCNQ2-CaM complex in closed conformation. QO-83 induces a negative shift in the voltage-dependent activation curve of KCNQ2 channels, increasing the channel's voltage sensitivity. QO-83 can be used for the research of epilepsies .
Cat. No.: HY-183335
Anticancer agent 321 is a Smoothened (SMO) inhibitor with a human IC50 of 0.12 μM, enhanced aqueous solubility, good plasma and metabolic stability, moderate therapeutic index, preliminary safety profile, and moderate oral bioavailability in rats.Anticancer agent 321 binds to SMO’s 7-transmembrane helical channel, forming hydrogen bonds with Asp384 and hydrophobic/π-π interactions with His470, Phe391, Tyr394, stabilizing SMO’s inactive conformation to inhibit Hedgehog/GLI signaling.Anticancer agent 321 inhibits proliferation, suppresses colony formation, induces apoptosis, and downregulates Hedgehog/GLI pathway target genes GLI1, GLI2, Ptch1, HHip in cancer cells.Anticancer agent 321 inhibits tumor growth, downregulates Ki67 and SOX2, and upregulates cleaved-caspase 3 in tumor tissues.Anticancer agent 321 can be used for the research of cutaneous squamous cell carcinoma .
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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
