less active enantiomer

Bay 41-4109 less active enantiomer shows less activity than Bay 41-4109. BAY 41-4109 is a potent HBV inhibitor (IC50: 53 nM).

Duvelisib (R enantiomer) hydrochloride (INK1197 R enantiomer HCl) is a PI3K inhibitor. Duvelisib (R enantiomer) hydrochloride is the less active enantiomer of Duvelisib.

(R)-Q-VD-OPh is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible inhibitor of pan-caspase, with potent antiapoptotic properties.

ARS-1630 is a mutant K-ras G12C inhibitor. It is a less active enantiomer of ARS-1620.

(-)-Taxifolin is the less active enantiomer of Taxifolin, demonstrating vital anti-tyrosinase activity and notable inhibition against collagenase (IC50 = 193.3 μM). It is valued as an essential natural compound showing antifibrotic potential, while also acting as a capable free radical scavenger and possessing antioxidant capacity.

(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special inhibitor of Mcl-1(IC50 of 1.81 nM).

Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib which is a selective MEK inhibitor.

Nazartinib is an EGFR inhibitor. Nazartinib S-enantiomer is the less active S-enantiomer of Nazartinib.

Tyrphostin B44, (+) enantiomer is an inhibitor of epidermal growth factor receptor (EGFR) kinase with IC50 of 0.86 μM and has less active than the (-) enantiomer.

R-(-)-Niguldipine hydrochloride is a L-type Ca2+ channel blocker; potassium agonist that activates Ca2+-activated maxi K-channel; alpha1A-adrenoceptor antagonist; antihypertensive agent; Less active enantiomer.

Umbralisib R-enantiomer (RP5264 R-enantiomer) is a delta inhibitor of PI3K and a less active enantiomer of TGR-1202. The IC50 of Umbralisib R-enantiomers against δPI3 kinase is at least 20 times lower than that of the inhibitors against other PI3K isoforms (A, β, and γ).

Fulvestrant R enantiomer is the less active R enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.

(3S,4S)-Tofacitinib, a less active enantiomer of tofacitinib, is a Janus kinases inhibitor.

(R)-Citalopram oxalate is a less active enantiomer of Escitalopram Oxalate. Escitalopram Oxalate is a potent and selective serotonin reuptake inhibitor.

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

(R)-Nicardipine is the less active R enantiomer of Nicardipine. Nicardipine is a blocker of calcium channel(IC50 of 1 μM for blocking cardiac calcium channels).

(S)-Tenofovir ((S)-PMPA) is the less active S-enantiomer of Tenofovir which is a nucleotide reverse transcriptase inhibitor.

(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC 50 >1μM for mGluR5 receptor [1] . BMS-984923 is a potent mGluR5 silent allosteric modulator [2] .

(S)-Sitagliptin phosphate, the less active S-enantiomer of Sitagliptin phosphate, is a high-potency inhibitor of DPP4. It exhibits an IC50 of 19 nM in Caco-2 cell extracts.

(S)-GNE-140 is the less active enantiomer of GNE-140.

(R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib, and Pirtobrutinib is a highly selective and non-covalent next generation BTK inhibitor. Pirtobrutinib (LOXO-305) effectively inhibits diverse BTK C481 substitution mutations[1].

Firsocostat S enantiomer is the less active S enantiomer of Firsocostat.

(R,S)-Ivosidenib is the less active enantiomer of Ivosidenib .

ADU-S100 (MIW815) enantiomer ammonium salt is the less active enantiomer of ADU-S100. ADU-S100 is an activator of the stimulator of interferon genes (STING).

(R)-MLN-4760, the R-enantiomer of MLN-4760, functions as an ACE2 inhibitor and exhibits a half maximal inhibitory concentration (IC50) of 8.4 μM, identifying it as the less active isomer.

(R)-Funapide ((R)-TV 45070), the less active R-enantiomer of Funapide, acts as a potent Nav1.7 sodium channel blocker, primarily utilized in pain research [1].

(3R,4S)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib is a JAK3 inhibitor(IC50 : 1 nM).

(3S, 4S)-PF-06459988 is the less active S enantiomer of PF-06459988, which is a potent irreversible inhibitor of T790M mutant epidermal growth factor receptor (EGFR). PF-06459988 exhibits excellent selectivity against EGFR wild-type due to its minimally reactive electrophile, which reduces the likelihood of off-target labeling.

PD-1-IN-20 is the less active enantiomer of PD-1-IN-1.

(R)-Propranolol hydrochloride (Dexpropranolol hydrochloride) is the less active enantiomer of the anti-adrenoceptor (β-adrenoceptor) antagonist propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist with a high affinity for β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively.

N(G)-Nitro-D-arginine methyl ester (D-NAME) is the less active enantiomer of the nitric oxide (NO) synthase inhibitor N(G)-nitro-L-arginine methyl ester . D-NAME was initially thought to be inactive and was often used as a negative control for L-NAME. Later studies showed that D-NAME (40 mg/kg/day in rats) can have similar but less pronounced effects as L-NAME (40 mg/kg/day in rats) in the cardiovascular system, particularly at long-term timepoints. D-NAME (3-10 µg/mouse) had no effect on nociception in mice assessed using the tail flick test.

(R)-SCH 42495 is the less active enantiomer of SCH 42495. SCH 42495 is an orally active inhibitor of neutral metalloendopeptidase (NEP), with antihypertensive effect.

(3S,4R)-Tofacitinib is an less active enantiomer of Tofacitinib. Tofacitinib is a JAK3 inhibitor(IC50 : 1 nM).

(2S,3R)-LP99 is a less active enantiomer of LP99.

(-)-Camphoric acid (L-Camphoric acid) is a less active enantiomer of Camphoric acid which induces GluR expression.

(R)-Plevitrexed is a less active enantiomer of Plevitrexed. Plevitrexed is an orally active and potent inhibitor of thymidylate synthase (TS).

(S)-Nicardipine is the less active S enantiomer of Nicardipine. Nicardipine is a blocker of calcium channel(IC50 of 1 μM for blocking cardiac calcium channels).

(R)-eIF4A3-IN-2, a less active enantiomer of eIF4A3-IN-2, is a highly selective and noncompetitive inhibitor of the eukaryotic initiation factor 4A-3 (eIF4A3) with an IC50 of 110 nM.

SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is an inhibitor of PIK3C3/Vps34.

(R)-Lanicemine ((R)-AZD6765), the less active R-enantiomer of Lanicemine, is a low-trapping NMDA channel blocker, exhibiting a binding affinity (Ki) of 0.56-2.1 μM for the NMDA receptor and inhibitory concentrations (IC50s) of 4-7 μM and 6.4 μM in CHO and Xenopus oocyte cells, respectively. It has been associated with antidepressant effects [1].

Firsocostat S enantiomer (ND-630 S enantiomer) is the less active S enantiomer of Firsocostat. Firsocostat is an acetyl-CoA carboxylase ( ACC ) inhibitor.

(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent agonist of α4β2 nAChR.

(S)-3'-hydroxy-Blebbistatin is a more stable and less phototoxic derivative of (–)-blebbistatin, retaining the latter's properties as a selective, cell-permeable inhibitor of non-muscle myosin II ATPases. Unlike its predecessor, (S)-3'-hydroxy-Blebbistatin exhibits reduced fluorescence, improving its utility in live cell imaging applications by diminishing degradation into cytotoxic intermediates under blue light exposure (450-490 nm). It effectively inhibits the Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB across various species with IC50 values ranging from 0.5-5 µM and shows minimal inhibition against smooth muscle myosin with an IC50 of 80 µM. This compound plays a critical role in preventing apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells, mirroring the active (–)-blebbistatin enantiomer in mechanism and efficacy.

Fulvestrant S enantiomer is the less active S enantiomer of Fulvestrant. Fulvestrant is a potent estrogen receptor antagonist with an IC50 of 9.4 nM.

(3S,4S)-A2-32-01, a less active (S,S)-enantiomer of A2-32-01. A2-32-01 is a potent caseinolytic protein proteases (ClpP) inhibitor .

(8R,9S)-Talazoparib is Talazoparib enantiomer , less active than Talazoparib on the inhibition of PARP1 (IC50: 144 nM).

(-)-Bornyl acetate (L-(-)-Bornyl acetate) is a less active enantiomer of (+)-Bornyl acetate. (-)-Bornyl acetate isolates from hyssop oil and possesses antifungal activity. (-)-Bornyl acetate shows highly active whitening and antioxidant activities, has potential applications in cosmeceutical materials. (-)-Bornyl acetate downregulated the levels of proinflammatory cytokines in vitro and in vivo; reduced the number of total cells, neutrophils, and macrophages in BALF; attenuated the histologic alterations in the lung; decreased the wet-to-dry weight ratio in BALF; and suppressed NF-kappa-B inhibitor alpha, extracellular regulated protein kinases, c-JunN-terminal kinase, p38 mitogen-activated protein kinase activation.

l-Atabrine dihydrochloride displays antiprion activity. l-Atabrine dihydrochloride is a less active enantiomer of quinacrine.

(R)-BAY-85-8501 is the less active enantiomer of BAY-85-8501. BAY-85-8501 is a selective and potent Human Neutrophil Elastase (HNE)inhibitor(IC50 of 65 pM).