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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
960 Results for "
manner
" in MedChemExpress (MCE) Product Catalog:
Products (960)
960 Results for "manner" in MCE Product Catalog:
Cat. No.: HY-W052508S
CAS No.: 1189866-35-0
Synonyms: N-Desalkylquetiapine-d8
Cat. No.: HY-W338810S
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S-(5'-Adenosyl)-L-methionine- 13C5 sulfate is the 13C-labeled S-(5'-Adenosyl)-L-methionine chloride (HY-W338810). S-(5'-Adenosyl)-L-methionine chloride is the endogenous methyl donor in the methionine cycle and numerous methylation reactions, including protein methylation. S-(5'-Adenosyl)-L-methionine chloride can activate cardiac ryanodine receptor RyR2 in a concentration-dependent manner, enhancing the affinity of RyR2 for ryanodine. The Kd of S-(5'-Adenosyl)-L-methionine chloride with MetJ in Escherichia coli is 0.18 mM. S-(5'-Adenosyl)-L-methionine chloride can cause changes in the methylation index of Cisplatin (HY-17394)-sensitive and Cisplatin-resistant ovarian cancer cells. S-(5'-Adenosyl)-L-methionine chloride can be used for methylation-related research .
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PPZ2 is a diacylglycerol (DAG)-activated TRPC3/TRPC6/TRPC7 channel activator with activity in promoting neuronal development and survival. PPZ2 activates recombinant TRPC3/TRPC6/TRPC7 channels in a dose-dependent manner without affecting other TRPC channels. PPZ2 elicits cation currents and calcium ion (Ca(2+)) influx in cultured central neurons. PPZ2 is able to induce BDNF-like neurite outgrowth and neuroprotection, an effect that disappears after TRPC3/TRPC6/TRPC7 knockdown or inhibition. PPZ2 also increases the activation of the calcium-dependent transcription factor cAMP response element binding protein. The effects of PPZ2 suggest that calcium signaling mediated by activation of DAG-activated TRPC channels plays an important role in its neurotrophic effects .
Cat. No.: HY-121501
CAS No.: 121024-51-9
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Tyrostatin is a peptide inhibitor isolated from Kitasatospora sp. 55. It has a Ki value of 6 nM against serine carboxyl protease (PSCP) from Pseudomonas sp. 101, a Ki value of 2.1 nM against carboxyl protease (XSCP) from Xanthomonas sp. T-22, and a Ki value of 2.6 nM against carboxyl protease (PCP) from Pseudomonas sp. 101. Tyrostatin forms a reversible covalent hemiacetal bond with Ser287 at the active site of PSCP, where Tyr at the P1 position and Leu at the P2 position occupy the S1-S4 subsites of the enzyme. Tyrostatin inhibits the activity of XSCP, specifically blocks the autocatalytic maturation process of PCP precursor under acidic conditions, and also inhibits the protease activity of mature and recombinant PCP in a dose-dependent manner. Tyrostatin does not inhibit KSCP or alcohol-resistant protease J-4, and can serve as a tool for identifying the catalytic residues of PCP .
Cat. No.: HY-126855S
CAS No.: 1332881-66-9
Synonyms: 7-Sulfocholic acid-d4
Cat. No.: HY-138074
CAS No.: 93074-04-5
Synonyms: 5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
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CCW16 is a non-selective cysteine-reactive covalent ligand and an RNF4 E3 ubiquitin ligase recruiter with an IC50 of 1.8 μM against human RNF4[. CCW16 covalently modifies accessible cysteine residues on RNF4, PRDX1, PRDX2, and PRDX6, attenuating the peroxide-scavenging activity of peroxiredoxins. CCW16 induces oxidative stress through upregulation of HMOX1 and NRF2, and triggers ferroptosis via lipid peroxidation and ROS signaling pathways in an RNF4-independent manner. CCW16 serves as an RNF4-recruiting moiety; it does not induce RNF4 degradation when used alone and can be used to synthesize protein degraders, such as the PROTAC compound CCW 28-3 (HY-156774). CCW16 can be used for research on acute myeloid leukemia and hepatocellular carcinoma .
Cat. No.: HY-163854
CAS No.: 3048341-44-9
HSP70-IN-6 (JL-15) is an inhibitor of Hsp70-Bim protein-protein interaction, with an IC50 value of 0.07 μM against Hsp70-Bim PPI, an IC50 of 4.89 μM and a Kd of 0.123 μM for BimBH3-stimulated Hsp70 ATPase activity. HSP70-IN-6 selectively blocks the binding of Hsp70-Bim without affecting the Hsp70-Bag3 interaction, and inhibits BimBH3-stimulated Hsp70 ATPase activity but has no impact on basal ATPase activity. HSP70-IN-6 induces apoptosis (apoptosis) in chronic myeloid leukemia cells in an Hsp70-Bim-dependent manner. HSP70-IN-6 can be used in research related to chronic myeloid leukemia .
Cat. No.: HY-175870A
CAS No.: 3024878-21-2
(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer .
Cat. No.: HY-179433
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PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer .
Cat. No.: HY-182066
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Photosensitizer-9 is an iridium (III)-based photosensitizer with anti-melanoma activity. Photosensitizer-9 exhibits significant phototoxicity (IC50=0.98 μM) and an ideal phototoxicity index (PI=3.05). Under light irradiation, Photosensitizer-9 generates large amounts of intracellular •OH in an oxygen-independent manner. Photosensitizer-9 mediates photodynamic therapy under hypoxic conditions and synergistically activates PANoptosis (by upregulating cleaved Caspase-3, GSDMD-N, p-MLKL), ferroptosis (by disrupting the GSH-GPX4-LPO axis), apoptosis, pyroptosis and necroptosis in melanoma cells. Photosensitizer-9 induces immunogenic cell death by promoting the release of damage-associated molecular patterns under hypoxic conditions and increases the maturation rate of dendritic cells. Photosensitizer-9 reduces tumor volume in melanoma-bearing mice. Photosensitizer-9 is applicable to relevant studies on melanoma .
Cat. No.: HY-184290
CAS No.: 3062852-59-6
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PRMT5-IN-56 is a PRMT5⋅MTA complex inhibitor with an IC50 of 0.2 nM, oral activity, and blood-brain barrier penetration. PRMT5-IN-56 inhibits PRMT5 methyltransferase activity in an MTA-cooperative manner, suppresses symmetrical dimethylarginine levels in MTAP-deficient cells. PRMT5-IN-56 suppresses proliferation of MTAP-deleted cancer cells with high selectivity over MTAP-wild type cells. PRMT5-IN-56 induces dose-dependent tumor growth inhibition in subcutaneous xenograft models, inhibits intracranial tumor progression, and prolongs survival in orthotopic brain xenograft models. PRMT5-IN-56 exhibits high intrinsic permeability, good oral bioavailability, and a high brain-to-plasma ratio. PRMT5-IN-56 can be used for the research of MTAP-deleted cancers and glioblastoma .
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Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect .
Antazoline phosphate is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline phosphate can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline phosphate can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline phosphate can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline phosphate also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline phosphate has anti-arrhythmic effect in acute myocardial infarctions. Antazoline phosphate can be studied in research for cardiovascular diseases, and HBV .
Cat. No.: HY-N0390S3
CAS No.: 2123439-02-9
Synonyms: L-Glutamic acid 5-amide-13C5,15N2,d5
Cat. No.: HY-N0390S6
CAS No.: 285978-14-5
Synonyms: L-Glutamic acid 5-amide-13C5,15N2
Cat. No.: HY-N0390S7
Synonyms: L-Glutamic acid 5-amide-15N2,d5
Cat. No.: HY-182820
CAS No.: 3086041-35-9
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YZ-836P is a Protein arginine methyltransferase 5 (PRMT5) targeting agent. YZ-836P promotes ubiquitination and proteasomal degradation of PRMT5 in a cereblon (CRBN)-dependent manner, which in turn reduces levels of its downstream target KLF5. YZ-836P induces G1 phase cell cycle arrest in triple-negative breast cancer cells. YZ-836P induces Apoptosis in triple-negative breast cancer cells. YZ-836P exerts cytotoxic effects on triple-negative breast cancer cells. YZ-836P inhibits the growth of triple-negative breast cancer patient-derived organoids. YZ-836P inhibits the growth of triple-negative breast cancer xenografts in nude mice. YZ-836P can be used for the research of triple-negative 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
