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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
122 Results for "
time-dependent
" in MedChemExpress (MCE) Product Catalog:
Products (122)
122 Results for "time-dependent" in MCE Product Catalog:
Cat. No.: HY-131731
CAS No.: 2353563-15-0
PROTAC STK4 Degrader-1 is a cereblon-recruiting STK4 PROTAC degrader. PROTAC STK4 Degrader-1 mediates ubiquitination and proteasomal degradation of STK4, induces dose- and time-dependent downregulation of STK4 in cancer cells, and exhibits reduced cytotoxicity in cereblon-knockout cells. PROTAC STK4 Degrader-1 can be used in research related to multiple myeloma .
Cat. No.: HY-108341AR
CAS No.: 1469284-79-4
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PF-06424439 methanesulfonate (Standard) is the analytical standard of PF-06424439 (methanesulfonate) (HY-108341A). This product is intended for research and analytical applications. PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
Cat. No.: HY-184377
CAS No.: 166181-63-1
Synonyms: IQB-9302
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Ipravacaine (IQB-9302) is a long-acting amide-based local anesthetic. Ipravacaine blocks open-state hKv1.5, with stereoselective, time-dependent and voltage-dependent inhibitory effects, and exerts stronger activity on the R (+) enantiomer. Ipravacaine blocks Kv2.1, Kv4.3 and HERG potassium channels. Ipravacaine induces negative chronotropic effects, increases mean arterial pressure, and exhibits vasodilatory effects at high concentrations .
Cat. No.: HY-181320
CAS No.: 2653338-65-7
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PROTAC EZH2 Degrader-19 (compound 6) is a is a PROTAC protein degrader targeting EZH2 with an IC50 of 15.00 nM. PROTAC EZH2 Degrader-19 induces strong degradation of all PRC2 subunits (EZH2, SUZ12, EED, RbAp48) in a concentration- and time-dependent manner.PROTAC EZH2 Degrader-19 exhibits antiproliferative effects in cancer cells.PROTAC EZH2 Degrader-19 can be used for the research of cancer .
Cat. No.: HY-182612
CAS No.: 2307429-54-3
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SRI-35241 is a thrombospondin TSP-1 inhibitor with a pIC50 of 8.12 nM against human targets. SRI-35241 inhibits the binding of TSP-1 to latent transforming growth factor-β-associated peptide (LAP) and blocks the activation of TGF-β. SRI-35241 shows a certain time-dependent property, with a plasma half-life of 1.8 h after intravenous administration. SRI-35241 can be used for the research of multiple myeloma and fibrotic diseases .
Cat. No.: HY-P992392
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Cat. No.: HY-179383
DprE1-IN-14 (Compound 77) is a DprE1 inhibitor, with an IC50 value of 2.5 nM for M. tb. DprE1-IN-14 exhibits anti-tuberculosis activity, with an MIC₉₀ of 0.3 μM for the M. tb mc26230 strain. DprE1-IN-14 mainly shows bacteriostatic activity, demonstrating a time-dependent bactericidal effect at 10-fold MIC concentrations. DprE1-IN-14 can be used in anti-tuberculosis research .
Cat. No.: HY-180969
CAS No.: 2378581-37-2
SIAIS056 is a BCR-ABL PROTAC degrader with a DC50 value of 0.18 nM. SIAIS056 time-dependently inhibits the BCR-ABL signaling pathway, accompanied by decreased phosphorylation of BCR-ABL and the downstream molecules STAT5 and CRKL in K562 cells. SIAIS056 induces the degradation of several clinically relevant resistance-conferring mutations of BCR-ABL. SIAIS056 exhibits anti-proliferative activity and induces substantial tumor regression in K562 xenograft models. SIAIS056 can be used for leukemia research .
Cat. No.: HY-181854
CAS No.: 3124583-65-6
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ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia .
Cat. No.: HY-186083
CAS No.: 36167-80-3
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Propylbenzilylcholine mustard (PrBCM) is an irreversible, covalently binding selective antagonist targeting rat cardiac muscarinic receptors, with a preference for muscarinic receptor subtypes that show low affinity for agonists. Propylbenzilylcholine mustard inactivates such receptors in a dose- and time-dependent manner in vitro, and its receptor selectivity remains stable across different ionic strengths and in GTP-containing buffer systems. Propylbenzilylcholine mustard can be applied to basic pharmacological studies on the structure and function of muscarinic receptors, especially focusing on the heterogeneity of cardiac muscarinic receptors and related cardiovascular pharmacological research .
Cat. No.: HY-P11849
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Cat. No.: HY-184653
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MS3-123 is an orally active PRMT1 inhibitor (IC50 = 11.4 nM) that selectively targets the unique Cys119 residue within the SAM-binding pocket. MS3-123 covalently binds to PRMT1 through a time-dependent irreversible mechanism and exhibits high selectivity over other PRMT family members and other methyltransferases. MS3-123 inhibits breast cancer cell proliferation, migration and invasion, and induces cell cycle arrest and apoptosis. MS3-123 is useful for breast cancer research .
Cat. No.: HY-123113
CAS No.: 65886-71-7
Synonyms: Kymarabine; Ara-AC; NSC 281272
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Fazarabine (Kymarabine; Ara-AC; NSC 281272) is an orally active, blood-brain barrier permeable DNA polymerase inhibitor and antitumor agent. Fazarabine interferes with DNA synthesis via intracellular activation into a triphosphate nucleotide that directly incorporates into DNA, inducing cytotoxicity, myelosuppression, as well as moderate nausea and vomiting. Fazarabine is resistant to deamination by cytidine-deoxycytidine deaminase and undergoes spontaneous aqueous degradation. Fazarabine exerts time-dependent, broad-spectrum activity against leukemia and solid tumors. Fazarabine can be used in research related to refractory malignancies, acute leukemia, and blast-phase chronic myeloid leukemia .
Cat. No.: HY-183378
CAS No.: 132259-06-4
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Cat. No.: HY-184880
CAS No.: 1410114-25-8
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BMS-986144 non-deuterated is the non-tritium form of BMS-986144 (HY-131905S). BMS-986144 is an orally active inhibitor of HCV NS3/4A protease. BMS-986144 binds to the active site of HCV NS3/4A protease and induces conformational changes in the protease. BMS-986144 reduces time-dependent CYP3A4 inhibition, exhibits hepatic microsomal metabolic stability, and undergoes oxidation of the macrocyclic linker chain. BMS-986144 can be used in studies related to hepatitis C virus infection .
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-121407A
CAS No.: 2180287-51-6
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(Rac)-Lateritin is an acyl-CoA:cholesterol acyltransferase (ACAT/SOAT) inhibitor, with IC50 values of 5.7 μM and 5.6 μM in rat liver, respectively. (Rac)-Lateritin exerts time-dependent irreversible enzyme inhibition that persists even after microsomal washing. (Rac)-Lateritin inhibits cholesterol ester formation in macrophages without altering triglyceride synthesis or other steps in oxidized low-density lipoprotein metabolism. (Rac)-Lateritin inhibits the growth of cancer cells, Gram-positive bacteria, and Candida albicans. (Rac)-Lateritin can be used in studies related to atherosclerosis, human solid tumors, mouse lymphocytic leukemia, as well as fungal and bacterial infections .
Cat. No.: HY-182382
CAS No.: 421579-95-5
Anticancer agent 311 is an apoptosis inducer and p53 modulator. Anticancer agent 311 increases p53 levels, activates cleaved caspase-3, reduces p-Cdc25C levels, and disrupts p-p44/42 MAPK phosphorylation. Anticancer agent 311 induces G2/M phase arrest, inhibits cancer cell viability in a concentration- and time-dependent manner, and exhibits low toxicity to non-cancer cells. Anticancer agent 311 prevents tumor growth and angiogenesis in mouse xenograft models without detectable toxicity. Anticancer agent 311 can be used for the research of lung cancer .
Cat. No.: HY-184837
CAS No.: 53772-82-0
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cis-Flupenthixol is an orally active dopamine receptor antagonist, with a Ki value of 1.4 nM for the Dopamine D-1 receptor and 0.74 nM for the Dopamine D-2 receptor. cis-Flupenthixol blocks dopamine receptors in the medial preoptic area and striatum, impairs male mating behavior, and reduces the concentrations of striatal dopamine metabolites. cis-Flupenthixol alters striatal acetylcholine concentrations in a time-dependent manner and enhances Apomorphine (HY-12723)-induced stereotyped behaviors. cis-Flupenthixol inhibits exploratory locomotor activity and triggers a compensatory increase in dopamine turnover in the striatum and limbic regions. cis-Flupenthixol can be used in studies related to tardive dyskinesia .
Cat. No.: HY-P992379
Synonyms: BAG3-H2L4
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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
