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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
320 Results for "
Complete
" in MedChemExpress (MCE) Product Catalog:
Products (320)
320 Results for "Complete" in MCE Product Catalog:
Cat. No.: HY-L035
5,148 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication. First, the risk of failure is lower. Second, the time frame for drug development can be reduced. Third, less investment is needed. Approved and clinical drugs, especially after phase I drugs, have identified bioactivities, good pharmacokinetic characteristics and safety which are suitable for drug repurposing.
MCE Drug Repurposing Compound Library contains 5,148 approved drugs and passed phase Ⅰclinical drugs, which have been completed extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties.
Cat. No.: HY-L022M
3,236 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication. First, the risk of failure is lower. Second, the time frame for drug development can be reduced. Third, less investment is needed. Approved drugs have identified bioactivities, good pharmacokinetic characteristics and safety which are suitable for drug repurposing.
MCE owns a unique collection of 3,236 approved compounds which have been completed extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties. The package of this library is 96-well microplate with peelable foil seal, which makes the screening process easier and faster.
Cat. No.: HY-L022
3,236 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication. First, the risk of failure is lower. Second, the time frame for drug development can be reduced. Third, less investment is needed. Approved drugs have identified bioactivities, good pharmacokinetic characteristics and safety which are suitable for drug repurposing.
MCE owns a unique collection of 3,236 approved compounds which have been completed extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties. MCE FDA-Approved Drug Library is a good tool for drug repurposing which could dramatically accelerate drug development.
Cat. No.: HY-148739
CAS No.: 2170679-42-0
Target:
Research Areas:
dBRD 9-A is a selective BRD9 PROTAC degrader. dBRD 9-A induces near complete BRD9 degradation dependent on E3 ubiquitin ligase CRBN and BRD9 bromodomain engagement, and drives loss of BRD9 chromatin binding genome-wide. dBRD 9-A downregulates oncogenic SS18-SSX-driven transcriptional programs, super enhancer-associated gene expression, and SS18-SSX1 super enhancer binding, and depletes GBAF complex members GLTSCR1/1L from SS18-SSX complexes. dBRD 9-A induces cell cycle arrest and increases apoptosis in synovial sarcoma cells. dBRD 9-A can be used for the research of synovial sarcoma .
Cat. No.: HY-184264
CAS No.: 1309199-94-7
CHVB-066 is an alphavirus non-structural protein nsP1 inhibitor that exhibits varying degrees of inhibitory activity against nsP1 of CHIKV and VEEV. CHVB-066 inhibits MTase and GTase activities and disrupts the capping process of viral RNA, including inhibiting CHIKV replication, reducing progeny viruses, and preventing cytopathic effects. It shows varying degrees of inhibitory activity against nsP1 of CHIKV and VEEV but lacks anti-SFV replication activity, displays cross-resistance with MADTP series compounds, and requires nsP2/nsP3 mutations to develop complete drug resistance. This inhibitor with varying inhibitory activity against nsP1 of CHIKV and VEEV can be widely applied to relevant studies on chikungunya virus infection and chikungunya fever .
Cat. No.: HY-D3577
Target:
Research Areas:
AF555 Picolyl Azide is a Fluorescent dye that enables site-specific fluorescent labeling via click chemistry. AF555 Picolyl Azide conjugates with the non-canonical amino acid N-propargyl-L-lysine introduced through ochre stop codon suppression via the copper (I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction, achieving labeling of hyperpolarization-activated cyclic nucleotide-gated HCN channels; its picolyl group accelerates the CuAAC reaction rate, thus completing labeling rapidly at room temperature and minimizing copper-induced cytotoxicity. AF555 Picolyl Azide forms covalent bonds with the alkynyl groups of nucleotide analogs through its azide moiety, labeling viral genomes containing 5-ethynyl-2'-deoxyuridine for visualization via fluorescence microscopy .
Cat. No.: HY-P87027
Synonyms: 20 kDa myosin light chain antibody; Human 20kDa myosin light chain (MLC2) mRNA Complete cds antibody; LC20 antibody; MGC3505 antibody; MLC 2 antibody; MLC-2C antibody; MLC2 antibody; MLY 9 antibody; MRLC1 antibody; MYL9 antibody; 20 kDa myosin light chain antibody; Human 20kDa myosin light chain (MLC2) mRNA Complete cds antibody; LC20 antibody; MGC3505 antibody; MLC 2 antibody; MLC-2C antibody; MLC2 antibody; MLY 9 antibody; MRLC1 antibody; MYL9 antibody; MYL9_HUMAN antibody; Myosin light chain 9 regulatory antibody; Myosin light polypeptide 9 regulatory antibody; myosin regulatory light chain 1 antibody; Myosin regulatory light chain 2 antibody; Myosin regulatory light chain 2 smooth muscle isoform antibody; Myosin regulatory light chain 9 antibody; Myosin regulatory light chain MRLC1 antibody; Myosin regulatory light polypeptide 9 antibody; Myosin RLC antibody; Myosin vascular smooth muscle light chain 2 antibody; MYRL2 antibody; OTTHUMP00000030857 antibody; smooth muscle isoform antibody;
Cat. No.: HY-P990774
CAS No.: 2768386-15-6
Synonyms: ASP-7266; TRAB-1; UPB-101
Target:
Research Areas:
Cat. No.: HY-118185
CAS No.: 115766-42-2
SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
Cat. No.: HY-W129441
CAS No.: 91281-32-2
Synonyms: N-Ac-4-S-CAP
Research Areas:
N-Acetyl-4-S-mercaptoaminophenol (N-Ac-4-S-CAP) is a compound that is selectively cytotoxic to melanocytes of black mouse hair follicles. It can cause 98% depigmentation of black mouse hair follicles. N-Ac-4-S-CAP can produce visible changes in hair follicle melanocytes 4 hours after intraperitoneal injection, including aggregation of melanin granules and nuclear condensation. Electron microscopy observations showed that it caused progressive destruction of melanocytes, including swelling of membranous organelles, nuclear condensation, and cytoplasmic vacuolation, ultimately leading to complete cell necrosis. N-Ac-4-S-CAP has a specific cytotoxic effect on melanocytes that actively produce eumelanin, but may not affect precursor or dormant melanocytes. These properties suggest that N-Ac-4-S-CAP may have potential application value in the treatment of melanoma or skin whitening.
Cat. No.: HY-L022P
3,663 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication. First, the risk of failure is lower. Second, the time frame for drug development can be reduced. Third, less investment is needed. Approved drugs have identified bioactivities, good pharmacokinetic characteristics and safety which are suitable for drug repurposing.
MCE owns a unique collection of 3,663 approved compounds which have been completed extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties. MCE FDA-Approved Drug Library Plus, with more powerful screening capability, further complements FDA-Approved Drug Library (HY-L022) by adding some compounds with low solubility or solution stability (Part B) to this library. All those supplementary are supplied in powder form.
Cat. No.: HY-188120
Research Areas:
AZD5335 is an ADC targeting FRα, with an IC50 of 10.6 nM against human FRα. AZD5335 specifically binds to FRα, mediates internalization and trafficking to lysosomal compartments, while delivering a topoisomerase I inhibitor payload that traps TOP1-DNA cleavage complexes. AZD5335 induces DNA damage response via the ATR, ATM, Chk1 and Chk2 signaling pathways, and increases the levels of phosphorylated KAP1, phosphorylated RPA, phosphorylated γH2AX, as well as PARP cleavage. AZD5335 exhibits bystander cytotoxicity against FRα-negative cells co-cultured with FRα-expressing cells. AZD5335 induces potent and durable responses and complete regression in ovarian cancer models, including models with low FRα expression and models resistant to Elahere, with enhanced efficacy when combined with Carboplatin, Bevacizumab or poly (ADP-ribose) polymerase inhibitors. AZD5335 can be used for ovarian cancer research .
Cat. No.: HY-L163
306 compounds
Traditional Chinese medicine provides abundant natural resources for medicinal compounds, which are often considered effective and safe for drug discovery. Traditional Chinese medicine is based on the principle of "multiple components, multiple targets, and multiple pathways", and naturally has multiple pharmacological effects. As herbal medicine, the secondary plant metabolites in Chinese herbal medicine play an important role in alleviating many diseases in Traditional medicine and folk use. Therefore, the identification of traditional Chinese medicine derived compounds is also an important process in drug development and a necessary factor in dissecting the overall mechanism of action of traditional Chinese medicine. FDA listed compounds have completed extensive preclinical and clinical studies, exhibiting good biological activity, safety, and bioavailability.
MCE designs a unique collection of 306 FDA/EMA/NMPA/PMDA etc-approved traditional Chinese medicine active compounds, including flavonoids, polyphenols, alkaloids, terpenoids, and other structural types. It is a good tool for drug reuse and screening drugs from traditional Chinese medicine sources.
Cat. No.: HY-178061
CAS No.: 2598870-24-5
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
Cat. No.: HY-L035P
6,142 compounds
New drug development is a time-consuming and high-cost process. Drug repurposing (also called drug repositioning, reprofiling or re‑tasking) offers various advantages over developing an entirely new drug for a given indication. First, the risk of failure is lower. Second, the time frame for drug development can be reduced. Third, less investment is needed. Approved and clinical drugs, especially after phase I drugs, have identified bioactivities, good pharmacokinetic characteristics and safety, which are suitable for drug repurposing.
MCE Drug Repurposing Compound Library plus contains 6,142 approved and passed phase I clinical drugs, which have been completed extensive preclinical and clinical studies and have well-characterized bioactivities, safety and bioavailability properties.
MCE Drug Repurposing Compound Library plus, with more powerful screening capability, further complement MCE Drug Repurposing Compound Library (HY-L035) by adding some compounds with low solubility or stability (Part B) to this library. All those supplementary compounds are supplied in powder form.
Cat. No.: HY-L036
1,618 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE covalent inhibitor library contains 1,618 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.
Cat. No.: HY-132031
CAS No.: 2682939-53-1
Target:
Research Areas:
Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 is a drug-linker conjugate composed of a cleavable Val-Ala linker and the potent ADC cytotoxin PNU-159682 (HY-16700), which is applicable for ADC synthesis. When conjugated with an anti-CD46 antibody, Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 delivers its payload to CD46-expressing cells, while cathepsin B cleaves the Val-Ala linker to release the payload. ADCs synthesized from Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 drive durable responses in CD46-expressing patient-derived xenograft models of non-small cell lung cancer and colorectal cancer, and a single administration induces complete tumor regression in most models. Mal-Val-Ala-PAB (C2-glucuronic acid)-DMEA-PNU-159682 can be used in the research of non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-L908
1,244 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE Lead-like Covalent Screening Library offers a valuable resource of 1,049 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in drug discovery.
Cat. No.: HY-L036P
6,121 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE covalent inhibitor library contains 6,121 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.
MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.
Cat. No.: HY-184501
CAS No.: 486440-74-8
UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC50 of 695.30 nM and a KD of 114.3 nM for ULK1; it inhibits hERK1 with an IC50 of 179.90 nM and a KD of 114 nM for ERK1; it shows weak binding to ERK2 with a KD of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to 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
