Scientific Reviews
Product Guides
Blogs
Topics
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
539 Results for "
Pi-binding pocket
" in MedChemExpress (MCE) Product Catalog:
Products (539)
539 Results for "Pi-binding pocket" in MCE Product Catalog:
Cat. No.: HY-155583
Purity: 98.08%
Target:
Research Areas:
RNase L-IN-1 is a RNase L inhibitor with an IC50 of 15.9 μM. RNase L-IN-1 binds to the ATP-binding pocket of RNase L, and inhibits ribosomal RNA cleavage. RNase L-IN-1 can be used for the research of RNase L-associated cellular processes .
Synonyms: INT131
Target:
Research Areas:
AMG131 (INT131) is a potent non-thiazolidinedione (TZD) selective peroxisome proliferator-activated receptor γ modulator (SPPARM). AMG131 binds to PPARγ within the same binding pocket as the TZDs, but occupies a unique space in the pocket and contacts the receptor at distinct points from the TZDs. AMG131 is promising for research of type-2 diabetes mellitus .
Cat. No.: HY-173352
CAS No.: 868940-26-5
Target:
Research Areas:
USP7 activator 1 (compound MS-8) is an activator of USP7 by engaging the allosteric C-terminal binding pocket of USP7 .
Target:
Research Areas:
Necrostatin-34 (Nec-34), a RIPK1 kinase inhibitor, stabilizes RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain .
Research Areas:
R-10015, a broad-spectrum antiviral compound for HIV infection, acts as a potent and selective inhibitor of LIM domain kinase (LIMK) and binds to the ATP-binding pocket, with an IC50 of 38 nM for human LIMK1 .
Research Areas:
Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research .
Target:
Research Areas:
CS587 is a selective CaMK1D inhibitor that binds to the ATP-binding pocket but fails to protect cells from Aβ-induced toxic damage . CS587 is used in Alzheimer's disease-related research .
Cat. No.: HY-19628
CAS No.: 1638644-62-8
Target:
Research Areas:
OD36 is a RIPK2 inhibitor with an IC50 of 5.3 nM. OD36 is a macrocyclic inhibitor with potent binding to the ALK2 kinase ATP pocket. OD36 shows ALK2-directed activity with KDs of 37 nM .
Target:
Research Areas:
PF-06672131 is an alkynylated afatinib derivative and a small molecule probe that is reactive to cysteine. PF-06672131 is an inhibitor of epidermal growth factor receptor (EGFR) kinase that targets the ATP pockets of EGFR. PF-06672131 can be used for activity-based protein profiling studies .
Target:
Research Areas:
Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket .
Cat. No.: HY-122184
CAS No.: 34387-64-9
PET-16 is a selective HSP70 inhibitor that binds to an allosteric pocket of the substrate-binding domain. PET-16 inhibits the ability of HSP70 to cycle between ATP-bound and ADP-bound states. PET-16 induces apoptosis in multiple myeloma .
Cat. No.: HY-155583A
Purity: 99.56%
Target:
Research Areas:
RNase L-IN-1 trihydrochloride is a RNase L inhibitor with an IC50 of 15.9 μM. RNase L-IN-1 trihydrochloride binds to the ATP-binding pocket of RNase L, and inhibits ribosomal RNA cleavage. RNase L-IN-1 trihydrochloride can be used for the research of RNase L-associated cellular processes .
Target:
Research Areas:
3BrB-PP1 is an ATP-competitive analog. 3BrB-PP1 can specifically inhibit the activity of protein kinase with mutations in the ATP-binding pocket (mutation of Thr97 within Sty1’s ATP-binding pocket) .
Cat. No.: HY-139906
CAS No.: 2045891-59-4
Target:
Research Areas:
CXCL12 ligand 1 is the first ligand of the sY12-binding pocket on chemokine CXCL12.
Target:
Research Areas:
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
Target:
Research Areas:
MLT-747 is a potent, selective, allosteric inhibitor of MALT1, binds MALT1 in the allosteric Trp580 pocket, with an IC50 of 14 nM .
Target:
Research Areas:
EGFR/AURKB-IN-1 (compound 7) is a dual-targeted EGFR/AURKB inhibitor, and inhibits the phpsphorylations of L858R EGFR and AURKB with IC50s of 0.07 and 1.1, respectively. EGFR/AURKB-IN-1 occupies the hydrophobic region I or the αC-helix out pocket of EGFR and the back pocket of AURKB, inhibiting the growth, division and metastasis of tumor cells, thus can be used for cancer research .
PNU-292137 is an orally active, potent CDK2 inhibitor with IC50s of 37 nM and 92 nM for CDK2/cyclin A and CDK2/cyclin E, respectively. PNU-292137 makes interactions with the hydrophobic pocket at the back of the CDK2 ATP pocket. PNU-292137 efficiently inhibits tumor cell proliferation in human colon and prostate tumor cell lines. PNU-292137 exhibits antitumor activity (TGI>50%) in a mouse xenograft model .
-
-
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
