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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
218 Results for "
less active
" in MedChemExpress (MCE) Product Catalog:
Products (218)
218 Results for "less active" in MCE Product Catalog:
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1 Cited Publications
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CDK5-IN-1 is a potent CDK5 inhibitor with an IC50 less than 10 nM. CDK5-IN-1 is greater than 100-fold more active against CDK5 than CDK2. CDK5-IN-1 is used for kidney diseases research .
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1 Cited Publications
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YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM. YUKA1 has less inhibitory active on KDM5C (IC50 = 7.12 μM) and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 can increase H3K4me3 levels and inhibit cell proliferation. YUKA1 can be used for the research of cancer, such as lung and breast cancers .
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1 Cited Publications
Synonyms: (S)-IDO1-IN-5
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(S)-LY-3381916 ((S)-IDO1-IN-5; Example 1B) is an active S-isomer of LY-3381916. (S)-LY-3381916 binds to IDOL with an IC50 value less than 1.5 µΜ . LY-3381916 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1 .
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Selvigaltin (GB1211) is an orally active galectin-3 small molecule inhibitor with an IC50 value of 12 nM in rabbits, showing anti-tumor activity. Selvigaltin decreases galectin-3 levels in the liver and reduces biomarkers of liver function (AST, ALT, bilirubin), inflammation (cells foci) and fibrosis (PSR, SHG), as well as decreasing the mRNA and protein expression of several key inflammation and fibrosis biomarkers (IL6, TGFβ3, SNAI2, collagen). Selvigaltin restores T-cell activity and induces less tumors and metastasis .
Synonyms: (-)-MK-801 maleate
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(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
Cat. No.: HY-W394903
CAS No.: 1257705-09-1
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GS-829845 is a is a major, active metabolite of Filgotinib (HY-18300). GS-829845 is a JAK1 preferential inhibitor but is approximately 10-fold less potent than the parent and with a longer half-life .
Synonyms: ONO-6818; ONO-PO-736
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Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity .
Cat. No.: HY-17044A
CAS No.: 1261590-48-0
Synonyms: IPI-145 R enantiomer; INK1197 R enantiomer
Duvelisib R enantiomer is a PI3K inhibitor, which is the less active enantiomer of Duvelisib.
Cat. No.: HY-16950B
CAS No.: 174592-47-3
Synonyms: (E)-Afimoxifene
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(E)-4-Hydroxytamoxifen ((E)-Afimoxifene), the less active isomer of (Z)-4-hydroxytamoxifen, is an estrogen receptor modulator.
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Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM) .
Cat. No.: HY-40354D
CAS No.: 1092578-46-5
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(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
Synonyms: IND-58359 S enantiomer; (S)-(-)-R-115777
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Tipifarnib S enantiomer is the S-enantiomer of Tipifarnib. Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM. Tipifarnib S enantiomer is the less active isomer.
Cat. No.: HY-40354C
CAS No.: 1092578-47-6
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(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
Synonyms: (S)-LP352
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(S)-Bexicaserin ((S)-LP352) is the less active S-enantiomer of Bexicaserin (HY-15601). Bexicaserin is a 5-HT2C agonist with the potential to be used in the study of obesity and psychiatric-related diseases .
Synonyms: AMG-510 isomer
Sotorasib (AMG-510) isomer is the less active isomer of Sotorasib (AMG-510). AMG-510 is a potent KRAS G12C covalent inhibitor.
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LLY-284 is the diastereomer of LLY-283 with much less active. LLY-283 is a potent inhibitor of PRMT5. LLY-284 has the potential for the research of cancer diseases .
Synonyms: URB913 (enantiomer)
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ARN 077 enantiomer (19) is the less active enantiomer of ARN 077, with an IC50 of 3.53 μM for rat NAAA .
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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
