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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
524 Results for "
Isoforms
" in MedChemExpress (MCE) Product Catalog:
Products (524)
524 Results for "Isoforms" in MCE Product Catalog:
Cat. No.: HY-12491
CAS No.: 691388-62-2
PIK-C98 is a potent and selective PI3K inhibitor, with IC50s of 0.59, 1.64, 3.65, and 0.74 μM for α, β, δ, and γ isoforms, respectively. PIK-C98 inhibits all class I PI3Ks but has no effects on AKT or mTOR activity. PIK-C98 interferes with the ATP-binding pockets of PI3Ks by forming H-bonds and arene-H interactions with specific amino acid residues. PIK-C98 induces apoptosis by inhibiting PI3K. PIK-C98 can be used for the research of multiple myeloma .
Cat. No.: HY-126969
CAS No.: 870095-15-1
Target:
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C333H is a selective PPARγ modulator with insulin-sensitizing and hypoglycemic activities. C333H exhibits similar insulin-sensitizing effects to thiazolidinediones (TZDs) in diabetic mouse models without significantly increasing body weight or adipose tissue weight. C333H increases circulating high molecular weight adiponectin isoform levels in diabetic db/db mice, reduces serine phosphorylation of PPARγ 273 in brown adipose tissue, and selectively modulates the expression of specific PPARγ target genes in adipose tissue. Express. C333H exhibits weak recruitment of co-activators and weak dissociation of co-repressors in vitro. These properties suggest that C333H may be a potential inhibitor of type 2 diabetes .
Cat. No.: HY-146223A
Purity: 98.00%
(3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
PI5P4Ks-IN-2 is a inhibitor of phosphatidylinositol 5-phosphate 4-kinase γ (PI5P4Kγ). PI5P4Ks-IN-2 targets to PI5P4K isoforms with pIC50 values of <4.3 (PI5P4Kα), <4.6 (PI5P4Kβ), 6.2 (PI5P4Kγ), 0.32 (PI5P4Kγ+), respectively .
Cat. No.: HY-159852
CAS No.: 2971769-60-3
BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
Cat. No.: HY-167832
CAS No.: 2059104-90-2
Target:
JNK SGK ROCK Tau Protein MMP DNA/RNA Synthesis Pyruvate Kinase NF-κB COX NO Synthase Reactive Oxygen Species (ROS)
Research Areas:
PT109 is an orally active, blood-brain barrier permeable multi-kinase inhibitor. By inhibiting PTBP1, PT109 promotes the switch of pyruvate kinase isoform from PKM2 to PKM1, thereby effectively inhibiting the proliferation and migration of glioblastoma multiforme and inducing its reprogramming into oligodendrocytes. PT109 also targets and regulates key signaling molecules such as JNK, SGK1, GSK3β to exert neuroprotective effects including promoting neurogenesis, inducing synapse formation and alleviating neuroinflammation. In Alzheimer's disease models, PT109 exhibits significant efficacy in improving spatial learning ability, along with excellent in vivo pharmacokinetic properties. PT109 can be used to investigate metabolic reprogramming of glioblastoma multiforme and neuroprotective mechanisms of Alzheimer's disease .
Cat. No.: HY-173481
CDK9-IN-37 (Compound 24) is a CDK9 inhibitor (EC50: 5.5 nM) with weak inhibition on other CDK isoforms, showing high selectivity. CDK9-IN-37 has significant antiproliferative activity against acute myeloid leukemia MOLM-13 cells (IC50: 0.034 μM). CDK9-IN-37 inhibits the CDK9 signaling pathway, reduces the phosphorylation level of RNAP II CTD (Ser2), downregulates the anti-apoptotic protein McI-1, induces cell apoptosis, and arrests the cell cycle at the G2/M phase. CDK9-IN-37 can be used in the study of acute myeloid leukemia (AML) .
Cat. No.: HY-180803
Target:
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LH17, a Kaempferol (HY-14590) derivative, is a potent and selective PDE4 inhibitor (PDE4D2 IC50 = 73 nM, PDE4B2 IC50 = 190 nM). LH17 exhibits remarkable selectivity (>136-fold) against other PDE isoforms (PDE1B/2A/3A/5A/8A/9A/10A) (IC50 > 10000 nM), with the exception of PDE7A1 (IC50 = 300 nM). LH17 distinctly interacts with PDE4 M-pocket. LH17 demonstrates remarkable anti-fibrotic efficacy in both in vitro and in vivo models. LH17 can be used for idiopathic pulmonary fibrosis (IPF) research .
Cat. No.: HY-182245
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Anticancer agent 314 is a multi-target anticancer agent with tubulin polymerization inhibitory activity (IC50 = 6.35 μM) and human carbonic anhydrase IX (Ki = 27.1 nM) and XII (Ki 20.9 = nM) inhibitory activity. Anticancer agent 314 binds to the colchicine-binding pocket of tubulin and inhibits tumor-associated carbonic anhydrase isoforms via zinc coordination within enzyme active sites. Anticancer agent 314 induces G2/M phase cell cycle arrest, apoptosis via p53-dependent signaling, and broad-spectrum antiproliferative activity across multiple cancer cells. Anticancer agent 314 can be used for the research of cancer, such as leukemia, melanoma, ovarian cancer .
Cat. No.: HY-19482
CAS No.: 630100-90-2
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E7107 is a pre-mRNA spliceosome inhibitor and apoptosis (Apoptosis) inducer. E7107 binds to spliceosome-associated protein 130, inhibits spliceosome assembly and pre-mRNA splicing, regulates cellular protein expression, induces G1 and G2/M phase cell cycle arrest, triggers DNA damage, alters R-loop levels, reduces CHEK2 expression, impairs transcriptional elongation, and shifts MCL1 splicing toward pro-apoptotic isoforms. E7107 inhibits tumor growth in xenograft models and reduces leukemia burden. E7107 can be used in the research of advanced solid tumors, acute myeloid leukemia, T-cell acute lymphoblastic leukemia, and triple-negative breast cancer .
Cat. No.: HY-180057
CAS No.: 2649899-08-9
Target:
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α5β1 integrin-IN-1 is a potent and selective α5β1 integrin inhibitor with an IC50 value of approximately 0.4 nM (pIC50 = 9.4 M). α5β1 integrin-IN-1 disrupts the interaction between α5β1 integrin and fibronectin, thereby blocking smooth muscle tension transmission and α5β1 integrin-mediated cell adhesion. α5β1 integrin-IN-1 can be used in the research of asthma and allergic asthma.
Cat. No.: HY-180406
CAS No.: 1262495-12-4
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NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal .
Cat. No.: HY-181684
Research Areas:
PDE5/CA-IN-1 is a dual PDE5 and carbonic anhydrase (CA) inhibitor, with IC50 values of 0.41, 38.4, and 9.1 nM against PDE5, hCA II, and hCA VA, respectively. PDE5/CA-IN-1 inhibits multiple hCA subtypes associated with Alzheimer's disease. As a cytoprotective agent and oxidative stress alleviator, PDE5/CA-IN-1 reduces oxidative stress, and prevents recognition memory and working memory impairments. PDE5/CA-IN-1 is available for the research of Alzheimer's disease .
Cat. No.: HY-182333
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AChE-IN-112 is an acetylcholinesterase (AChE) inhibitor with an IC50 of 0.41 μM. AChE-IN-112 scavenges various reactive oxygen and reactive nitrogen species, including DPPH, ABTS, NO, hydroxyl and hydrogen peroxide free radicals. AChE-IN-112 can be used for the research of Alzheimer's disease .
Cat. No.: HY-183366
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HDAC1-IN-14 is an indole-based benzamide selective HDAC1 inhibitor with an IC50 of 77 nM. HDAC1-IN-14 acts as an antiproliferative agent, with GI50 values ranging from nanomolar to low micromolar levels in various cancer cells. HDAC1-IN-14 induces G0-G1 cell cycle arrest in colon cancer cells. HDAC1-IN-14 upregulates the expression of Caspase-3, Cyto-C and Bax, and downregulates the expression of AKT-1. HDAC1-IN-14 can be used in research related to leukemia, non-small cell lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer and breast cancer .
Cat. No.: HY-183606
Mycobacterium tuberculosis-IN-9 is an orally active Mycobacterium tuberculosis BioA inhibitor with a Ki value of 0.2 nM. Mycobacterium tuberculosis-IN-9 targets the biotin biosynthesis pathway. Mycobacterium tuberculosis-IN-9 inhibits the growth of Mycobacterium tuberculosis in mouse models and is effective against both drug-sensitive and drug-resistant strains. Mycobacterium tuberculosis-IN-9 can be used for the research of tuberculosis .
Cat. No.: HY-19480B
CAS No.: 1246200-39-4
Synonyms: BCX4208 succinate
Target:
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Ulodesine succinate (BCX4208 succinate) is a purine nucleoside phosphorylase (PNP) inhibitor, with an IC50 of 2.293 nM against human PNP, and low nanomolar IC50 values against mouse, rat and monkey PNP. Ulodesine succinate blocks the production of uric acid precursors, reduces serum uric acid levels, clears accumulated uric acid in the blood, and elevates the levels of purine nucleosides including guanosine. Ulodesine succinate reduces the counts of total lymphocytes, T lymphocytes and lymphocyte subsets, inhibits the proliferation of cancer cells and activated lymphocytes, and enhances vaccine immune responses. Ulodesine succinate can be used in research related to hyperuricemia and gout .
Target:
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CS640 (Compound 19) is a chemical probe and a calmodulin-dependent kinase inhibitor. CS640 inhibits CaMK1D, CaMK1B, CaMK1A, CaMK1G, MEK5, RIPK4, mLK3 and PIP5K1, with IC50 values of 8, 3, 1, 1, 25 nM, 5.69, 2.75 and 11.2 μM, respectively. CS640 blocks Aβ-induced hyperphosphorylation of tau protein at the Thr181 site, but fails to protect primary mouse cortical neurons from Aβ-induced toxic damage. CS640 is applicable to research related to Alzheimer's disease .
Cat. No.: HY-10214R
CAS No.: 908112-43-6
Synonyms: PF-04928473 (Standard)
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SNX-2112 (Standard) is the analytical standard of SNX-2112 (HY-10214). This product is intended for research and analytical applications. SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively . SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively .
Cat. No.: HY-19471
CAS No.: 1010440-84-2
(rac)-ZK-304709 is an isoform of ZK-304709 and is an orally active multi-targeted tumor growth inhibitor that inhibits multiple cell cycle-dependent kinases (CDKs), vascular endothelial growth factor receptor kinases (VEGF-RTKs), and platelet-derived growth factor receptor kinase β (PDGF-RTKβ). (rac)-ZK-304709 can dose-dependently inhibit the proliferation and colony formation of neuroendocrine tumor (NET) cells. (rac)-ZK-304709 directly acts on NET cells by inducing G2 cell cycle arrest and apoptosis, while reducing the expression of MCL1, survivin, and HIF1α. (rac)-ZK-304709 effectively controls tumor growth by inducing apoptosis and inhibiting tumor-induced angiogenesis, and may become a potential agent for inhibiting NET .
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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
