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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
443 Results for "
isoforms
" in MedChemExpress (MCE) Product Catalog:
Products (443)
443 Results for "isoforms" in MCE Product Catalog:
Cat. No.: HY-178913
CAS No.: 2734918-75-1
Research Areas:
Tyk2-IN-23 is a potent, orally active, selective TYK2 inhibitor (IC50 = 18 nM), exhibiting more than > 70-fold selectivity over JAK1/2/3 isoforms. Tyk2-IN-23 potently inhibits p-STAT3 in TYK2-dependent signaling activated by IFN-α and IL-10. Tyk2-IN-23 potently inhibits IFN-α-induced STAT1 phosphorylation in H9 cells. Tyk2-IN-23 can be used for the study of alopecia areata and allergic Rhinitis .
Cat. No.: HY-180526
CAS No.: 2055901-03-4
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PDE2A-IN-2 is a selective and brain-penetrant PDE2A inhibitor (Ki = 5.49 nM and 100 > fold selectivity over other PDE isoforms). The 11C-labeled PDE2A-IN-2 serves as a positron emission tomography (PET) tracer for brain imaging in patients with neurodegenerative diseases. PDE2A-IN-2 educes the radiotracer signal in PDE2A-rich regions in vitro. PDE2A-IN-2 exhibits low binding affinity in vivo. PDE2A-IN-2 can be used for neurodegenerative diseases .
Cat. No.: HY-183575
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JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia .
Cat. No.: HY-D3442
CAS No.: 3121565-89-4
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ALDH2 probe 5 is a ALDH2 isoform-selective fluorescent probe with an emission wavelength centered at 494 nm. ALDH2 probe 5 is a turn-on fluorescent substrate for ALDH2; in its unreacted aldehyde form, twisted intramolecular charge transfer (TICT) occurs, resulting in fluorescence quenching. After ALDH2 probe 5 is catalytically oxidized to carboxylate by ALDH2, TICT is inhibited and fluorescence is significantly enhanced. ALDH2 probe 5 enables highly sensitive quantitative imaging of ALDH2 activity in recombinant enzymes, live cells, blood, tissue homogenates, and the brains of living mice. ALDH2 probe 5 can be used for studies related to neuroinflammation .
Cat. No.: HY-U00237B
CAS No.: 200051-19-0
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L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
Cat. No.: HY-104048R
CAS No.: 1851373-36-8
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QC6352 (Standard) is the analytical standard of QC6352 (HY-104048). This product is intended for research and analytical applications. QC6352 is an orally active KDM4 inhibitor with anti-tumor and anti-proliferative activity. QC6352 has in vivo inhibitory effects on PDX models of breast and colon cancer and reduces the number of chemoresistant cell populations. QC6352 inhibits KDM4 different isoforms with IC50s of 104 nM (KDM4A), 56 nM (KDM4B), 35 nM (KDM4C), and 104 nM (KDM4D), respectively. QC6352 has moderate inhibitory activity against KDM5 with an IC50 of 750 nM (KDM5B) .
Cat. No.: HY-105353
CAS No.: 287173-08-4
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CEB-1604 is an NMDA receptor antagonist. CEB-1604 inhibits NMDA-induced currents in oocytes transfected with NMDA receptor isoforms (NR1/NR2A, NR1/NR2B, NR1/NR2C, NR1/NR2D) with IC50 values ranging from 5 to 12 μM. CEB-1604 abolishes NMDA-dependent epileptiform discharges in rat cortical wedge preparations and reduces the depolarizing effects of NMDA. CEB-1604 can be used in the research field of neurological damage diseases .
Cat. No.: HY-108642BR
CAS No.: 2518299-32-4
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AMG-548 dihydrochloride (Standard) is the analytical standard of AMG-548 (dihydrochloride) (HY-108642B). This product is intended for research and analytical applications. AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein Kinase 1 isoforms δ and ε .
Cat. No.: HY-134058S
Synonyms: Butylethylcarbinol-d4
Cat. No.: HY-115549
CAS No.: 1364692-88-5
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AMPK activator 18 is a potent allosteric activator of AMPK complexes containing the β2 isoform. AMPK activator 18activates α2-containing AMPK α2β2γ1 and α2β2γ3 complexes, with EC50 values of 17.2 and 82.1 nM. AMPK activator 18 stimulates β2-AMPK in cells, and glucose uptake by isolated skeletal muscle. AMPK activator 18 induces acetyl-coenzyme A carboxylase (ACC) and AMPK α-T172 phosphorylation. AMPK activator 18 can be used for the research of type 2 diabetes .
Cat. No.: HY-118030
CAS No.: 1257116-00-9
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RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2 isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .
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
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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-181710
LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer .
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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
