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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
52 Results for "
In vitro stability
" in MedChemExpress (MCE) Product Catalog:
Products (52)
52 Results for "In vitro stability" in MCE Product Catalog:
2
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Research Areas:
Ibuzatrelvir (PF-07817883), a second-generation, orally bioavailable, is SARS-CoV-2 main protease (M pro and 3CL pro) inhibitor with improved metabolic stability. Ibuzatrelvir has demonstrated pan-human coronavirus antiviral activity and off-target selectivity profile in vitro and in preclinical animal studies. Ibuzatrelvir is well tolerated with a safety profile similar to placebo and prevents viral infection and transmission. Ibuzatrelvir can be used to inhibit COVID-19 .
DPyPE is a neutral phosphatidylethanolamine lipid composed of a polyisoprene alkyl chain with two pyridine-containing phosphine ligands. DPyPE is mainly used in liposome formulations and to enhance the efficiency of gene delivery in vitro and in vivo. For example, DPyPE can be mixed with cationic lipids such as VC1052 (HY-156616) (in a 1:1 ratio) to form the vaccine adjuvant Vaxfectin (HY-142998). DPyPE assists VC1052 in binding to negatively charged pDNA to form a uniform liposome complex by regulating the fluidity and stability of the liposome membrane .
Cat. No.: HY-163099
CAS No.: 2928571-43-9
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P5 (PEG24)-VC-PAB-Exatecan is a TOP1 inhibitor payload with antibody-conjugation-dependent activity. Conjugation of P5 (PEG24)-VC-PAB-Exatecan with Trastuzumab (HY-P9907) generates a DAR8 antibody-drug conjugate (ADCs) with antibody-like pharmacokinetic properties. P5 (PEG24)-VC-PAB-Exatecan induces S-phase and G2-M-phase cell cycle arrest, DNA damage and apoptosis in target-positive tumor cells, and releases damage-associated molecular patterns (DAMP) related to immunogenic cell death (ICD). The ADCs prepared from it exert bystander killing effects on non-target tumor cells. ADCs based on P5 (PEG24)-VC-PAB-Exatecan exhibit linker stability in vitro and in vivo, show in vivo efficacy, and can be used in research related to HER2-positive cancers .
Cat. No.: HY-W133963
CAS No.: 9063-38-1
Cat. No.: HY-N10159
CAS No.: 60941-76-6
Target:
Cat. No.: HY-145815A
Purity: 98.40%
JPS014 TFA is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 TFA recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 TFA acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 TFA increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 TFA can be used for the research of colon cancer .
Cat. No.: HY-128947
CAS No.: 2270986-66-6
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CL2 Linker is a cleavableADC linker. CL2-SN-38 and CL2A-SN-38 are equivalent in agent substitution (~6), cell binding (Kd ~1.2 nM), cytotoxicity (IC50 ~2.2 nM), and serum stability in vitro (t1/2 ~20 hours) .
Cat. No.: HY-125209A
CAS No.: 2253744-57-7
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TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
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Dodecylamine (Laurylamine) is a compound that strongly destabilizes and inactivates L-(+)-pantoyl lactone dehydrogenase in vitro, can be used for assessing the enzyme's stability in biochemical assays .
Cat. No.: HY-163350
CAS No.: 3056445-53-2
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TUG-2208 (compound 42a) is a GPR84 agonist (pEC50=8.98) with low lipophilicity and good solubility, in vitro permeability and microsomal stability .
Cat. No.: HY-149920
CAS No.: 2857070-72-3
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Anticancer agent 98 (compound 12k) is a microtubule/tubulin-polymerization inhibitor (Kd=16.9 μM). Anticancer agent 98 exerts antiproliferative potency against tumor cells, exhibits anti-angiogenesis effect in vitro. Anticancer agent 98 exhibits good human and mouse liver microsomes stability with both t1/2>300 min .
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PB1 is a potent intracellular disulfide reducing agent with several advantages including good cell permeability, the ability to form a high intracellular concentration gradient, and stability. PB1 is a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 increases retinal ganglion cells survival after axotomy in vitro at nanomolar and picomolar concentrations. PB1 can be used for the research of neuroprotective .
Cat. No.: HY-145976
CAS No.: 133608-76-1
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m7GpppGpG is an unmodified trinucleotide cap analog with enhancer activity. When incorporated into mRNA, it effectively enhances translational efficiency, stability, and protein expression levels of the mRNA. m7GpppGpG can serve as a standard cap analog for in vitro mRNA synthesis to support antigen generation and presentation by dendritic cells, although its expression efficiency in dendritic cells is 20-fold lower than that of the m7GpppApG cap .
Cat. No.: HY-155732
CAS No.: 3032452-65-3
NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively .
Cat. No.: HY-145815
CAS No.: 2669785-76-4
JPS014 is a PROTAC degrader targeting HDAC1, HDAC2 and HDAC3, with DC50 values of 0.91 μM, 4.19 μM and 0.64 μM, respectively. JPS014 recruits the VHL E3 ligase to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS014 acts as a submicromolar inhibitor of the HDAC1-CoREST, HDAC2-CoREST and HDAC3-SMRT complexes in vitro. JPS014 increases the level of H3K56ac, reduces the stability of LSD1 and SIN3A, and induces cell apoptosis (apoptosis). JPS014 can be used for the research of colon cancer .
Cat. No.: HY-173623
CAS No.: 3057728-22-7
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EU 1622-240 is a biased positive allosteric modulator of GluN2B, GluN2C, and GluN2D, with EC50s of 0.57, 0.82, 1.1 μM respectively. EU 1622-240 has good physicochemical properties, in vitro stability, and permeability .
Cat. No.: HY-W419570
CAS No.: 478005-11-7
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(Rac)-BX 048 is a BX 048 racemate. BX 048 is a P2Y12 receptor antagonist. BX 048 inhibits ADP-induced platelet aggregation in human, dog and rat whole blood. BX 048 also inhibits Arachidonic acid (HY-109590) induced platelet aggregation (IC50 of 15 μM) .
Cat. No.: HY-16750
CAS No.: 1314795-11-3
Synonyms: GS-9669
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Radalbuvir (GS-9669) is a non-nucleoside inhibitor of nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp). Radalbuvir shows strong anti-HCV potency (GT1a intrinsic EC50 = 2.9 nM, GT1b EC50 = 6 nM) .
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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
