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Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
Prazobind (SZL 49), a prazosin analog, is a potent alpha 1-adrenoceptor blocker. Prazobind competes for alpha 1-adrenoceptor binding sites with a similar potency (IC50=1 nM) in tissues enriched in both the alpha 1A (hippocampus) and alpha1B (liver) subtypes .
Ficusonolide has significant antidiabetic activity with a possible mechanism of interaction with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.
PTP1B-IN-27 (Compound 7i) is an inhibitor of protein tyrosine phosphatase 1-B(PTP‐1B)(IC50=8.2 µM). PTP1B-IN-27 also inhibits α-Glucosidase (IC50=120 µM) and shows competitive inhibition (Ki=118 µM) .
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha1b and alpha 1c, respectively .
Rec 15/2615 hydrochloride is a potent and selective α-1B adrenoceptor antagonist with Ki values of 1.9 nM, 0.3 nM, 2.6 nM for α1A, α1B, α1D, respectively. Rec 15/2615 hydrochloride modulates vaginal smooth muscle contractility and genital engorgement .
Uncaric acid (6β,19α-Dihydroxyursolic acid) (compound 6) is a triterpene that can be found in Eriobotrya japonica. Uncaric acid shows anti HIV-1, HRV 1B, SNV activity .
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B(PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research .
Penpaxilloids A (Compound 1) is a non-competitive inhibitor of protein tyrosine phosphatase 1B(PTP1B) with an IC50 value of 8.60 μM. Penpaxilloids A can be isolated from the fungus Penicillium sp. ZYX-Z-143. Penpaxilloids A are also α-glucosidase (α-glucosidase) inhibitors and have anti-inflammatory activity .
MI 14 is a selective PI4KIIIβ inhibitor with IC50s of 54 nM, >100 μM, >100 μM for PI4KIIIβ, PI4KIIIα, PI4KIIα, respectively. MI 14 has antiviral activity against HCV 1b, CVB3, HRVM, HVC 2a .
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
α1b-AR antagonist 1 (Compound Cpd1) is a selective α1B-AR antagonist. Alpha1b-ar antagonist 1 can be used in the study of cardiovascular and central nervous system diseases .
6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer[1].
6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1(OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer .
L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.
Zolertine hydrochloride is an α-adrenoceptor antagonist with a pKi of 6.81 in rat liver (α1B-adrenoceptors) and 6.35 in rabbit liver (α1A-adrenoceptors) membranes .
(R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D,α1B and α1A receptors respectively.
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively .
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
(S)-Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Cirazoline hydrochloride (LD 3098 hydrochloride) is a potent competitive full α1A-adrenergic receptor (α1A-AR) agonist (Ki=120 nM) and only a partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR (Ki=660 nM) .
Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-,α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia .
Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-,α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-,α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia .
RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia .
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively .
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist with Ki values of 14.5, 43.3 nM for α1a-AR and α1b-AR, respectively. BODIPY FL prazosin also is a fluorescent ligand with the excitation and emission wavelengths are 485 and 535 nm, respectively. BODIPY FL prazosin can be used for study the differences in the subcellular localization of α1-adrenoceptor subtypes .
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent .
Naftopidil (Standard) is the analytical standard of Naftopidil. This product is intended for research and analytical applications. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-,α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia .
Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
BMY 7378 is a selective antagonist of α1D-adrenoceptor(α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist .
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A,α1B,α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
Silodosin (Standard) is the analytical standard of Silodosin. This product is intended for research and analytical applications. Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
PTP1B-IN-25 (Compound 19) is a PTP1B inhibitor with remarkable antiviral, antibacterial, and antidiabetic activities. PTP1B-IN-25 has IC50 values of 0.37 μM, 8.6 μM, 3.7 μM, and 29 μM against PTP1B, HIV, α-Glucosidase, and methicillin-resistant Staphylococcus aureus (MRSA) respectively .
(-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
Caffeoyltryptophan is a competitive PTP1B inhibitor, with an IC50 of 16.99 μM. Caffeoyltryptophan can also inhibit α-glucosidase, linoleic acid peroxidation and haemolysis. Caffeoyltryptophan can be used for the research of type 2 diabetes .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
LY393615 (NCC1048) is a novel neuronal Ca 2+ (calcium channel) and Na + channel (sodium channel) blocker with IC50s of 1.9 μΜ and 5.2 μΜ for α1A and α1B calcium channel subunits. LY393615 has good brain penetration and neuroprotective effects in models of in cerebral ischemia that can be used for neurological disease research .
EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively .
PDE4-IN-15 (compound 7b-1) is an inhibitor of PDE4 (IC50 = 0.17 μM) and has anti-TNF-α activity (EC50 = 0.19 μM). PDE4-IN-15 has a good skin permeability .
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
Ro 31-8220 is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
SIMR3030 is a potent SARS-CoV-2 PLpro inhibitor with an IC50 value of 0.0399 µg/mL. SIMR3030 shows antiviral activity. SIMR3030 decreases SARS-CoV spike, ORF1b, IFN-α, IL-6 mRNA expression. SIMR3030 exhibits a satisfactory safety profile in mice .
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker . Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites . Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases .
Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
Brexpiprazole (Standard) is the analytical standard of Brexpiprazole. This product is intended for research and analytical applications. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist with Ki values of 14.5, 43.3 nM for α1a-AR and α1b-AR, respectively. BODIPY FL prazosin also is a fluorescent ligand with the excitation and emission wavelengths are 485 and 535 nm, respectively. BODIPY FL prazosin can be used for study the differences in the subcellular localization of α1-adrenoceptor subtypes .
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC50 values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation .
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A,α1B,α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
Ficusonolide has significant antidiabetic activity with a possible mechanism of interaction with dipeptidyl peptidase-IV (DPP-IV), protein tyrosine phosphatase 1B (PTP-1B), α-glucosidase, and α-amylase.
Uncaric acid (6β,19α-Dihydroxyursolic acid) (compound 6) is a triterpene that can be found in Eriobotrya japonica. Uncaric acid shows anti HIV-1, HRV 1B, SNV activity .
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B(PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research .
Penpaxilloids A (Compound 1) is a non-competitive inhibitor of protein tyrosine phosphatase 1B(PTP1B) with an IC50 value of 8.60 μM. Penpaxilloids A can be isolated from the fungus Penicillium sp. ZYX-Z-143. Penpaxilloids A are also α-glucosidase (α-glucosidase) inhibitors and have anti-inflammatory activity .
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
(R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D,α1B and α1A receptors respectively.
Caffeoyltryptophan is a competitive PTP1B inhibitor, with an IC50 of 16.99 μM. Caffeoyltryptophan can also inhibit α-glucosidase, linoleic acid peroxidation and haemolysis. Caffeoyltryptophan can be used for the research of type 2 diabetes .
The A1BG/Alpha-1B-Glycoprotein protein forms a complex with CRISP3, indicating a potential functional association. This interaction prompts further exploration of its biological consequences and regulatory mechanisms. The precise roles and implications within cellular processes or physiological pathways require additional research for a comprehensive understanding. A1BG/Alpha-1B-Glycoprotein Protein, Human (HEK293, His) is the recombinant human-derived A1BG/Alpha-1B-Glycoprotein protein, expressed by HEK293 , with C-His labeled tag. The total length of A1BG/Alpha-1B-Glycoprotein Protein, Human (HEK293, His) is 474 a.a., with molecular weight of ~70-80 kDa.
RSK2 is a kinase downstream of ERK signaling and plays a critical role in mediating mitosis and stress responses. It activates transcription factors (CREB1, ETV1, NR4A1), affecting proliferation, survival and differentiation. RSK2 Protein, Human is the recombinant human-derived RSK2 protein, expressed by E. coli , with tag free. The total length of RSK2 Protein, Human is 341 a.a., .
In the Hippo signaling pathway, MOB1A acts as an important activator to control organ size and suppress tumors by regulating proliferation and apoptosis. MOB1A participates in the kinase cascade together with STK3/MST2 and STK4/MST1 to phosphorylate and activate LATS1/2, thereby affecting YAP1 oncoprotein and WWTR1/TAZ. MOB1A Protein, Human (His) is the recombinant human-derived MOB1A protein, expressed by E. coli , with C-6*His labeled tag.
RSK2 is a kinase downstream of ERK signaling and plays a critical role in mediating mitosis and stress responses. It activates transcription factors (CREB1, ETV1, NR4A1), affecting proliferation, survival and differentiation. RSK2 Protein, Human (His) is the recombinant human-derived RSK2 protein, expressed by E. coli , with N-6*His labeled tag. The total length of RSK2 Protein, Human (His) is 341 a.a., .
MAN1B1, integral to glycoprotein quality control, trims a single alpha-1,2-linked mannose from Man(9)GlcNAc(2), producing Man(8)GlcNAc(2). In the ERQC, elevated enzyme concentrations allow further trimming to Man(5-6)GlcNAc(2). This enzymatic function is crucial for glycoprotein processing and quality control in the endoplasmic reticulum, ensuring proper folding and maturation. MAN1B1 Protein, Human (HEK293, His) is the recombinant human-derived MAN1B1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of MAN1B1 Protein, Human (HEK293, His) is 594 a.a., with molecular weight of 58-80 kDa.
TNFRII (TNFRSF1B) protein has a high ability to bind with tumor necrosis factor-alpha (TNF-α). TNFRII has pro-apoptotic function. TNFRII recruits TRAF2, induces gene expression and intensively crosstalks with TNF-R1. TNFRII selectively enhances the induction of apoptosis by the death receptor TNFRI. TNF RII/TNFRSF1B Protein, Human (183a.a, HEK293, mFc) is expressed by HEK293 and has a transmembrane region (P24-T206) with mFc tag at the C-terminus.
TNFRII (TNFRSF1B) protein has a high ability to bind with tumor necrosis factor-alpha (TNF-α). TNFRII has pro-apoptotic function. TNFRII recruits TRAF2, induces gene expression and intensively crosstalks with TNF-R1. TNFRII selectively enhances the induction of apoptosis by the death receptor TNFRI. TNFRII Protein, Human (174a.a, HEK293, His) is expressed by HEK293 and has a transmembrane region (K288-S461) with 6*His tag at the C-terminus.
The animal-free TNF beta protein acts as a homotrimeric cytokine that binds TNFRSF1A/TNFR1, TNFRSF1B/TNFBR, and TNFRSF14/HVEM. Animal-Free TNF beta Protein, Mouse (His) is the recombinant mouse-derived animal-FreeTNF beta protein, expressed by E. coli , with N-His labeled tag. The total length of Animal-Free TNF beta Protein, Mouse (His) is 169 a.a., with molecular weight of ~19.36 kDa.
Serpin A1b Protein, a vigilant guardian in cellular regulation, adeptly inhibits elastase, providing formidable defense against its enzymatic activity. Beyond this specialization, Serpin A1b shows moderate affinity for plasmin and thrombin, highlighting its versatility in interacting with various serine proteases. As a multifaceted sentinel, Serpin A1b contributes to the nuanced orchestration of proteolytic processes within cellular landscapes. Serpin A1b Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived Serpin A1b protein, expressed by HEK293 , with C-hFc labeled tag. The total length of Serpin A1b Protein, Mouse (HEK293, Fc) is 389 a.a., with molecular weight of ~70.2 kDa.
The MAN1A2 protein is crucially involved in the maturation of Asn-linked oligosaccharides, which in turn trims α-1,2-linked mannose residues from Man(9)GlcNAc(2) to generate Man(5)GlcNAc(2). During glycosylation, MAN1A2 plays a key role in the progressive trimming of mannose residues that are essential for generating mature glycan structures. MAN1A2 Protein, Human (HEK293, His) is the recombinant human-derived MAN1A2 protein, expressed by HEK293 , with N-His labeled tag. The total length of MAN1A2 Protein, Human (HEK293, His) is 584 a.a., with molecular weight of ~69 KDa.
IFN-alpha 1a/IFNA1 Protein, produced by macrophages, demonstrates robust antiviral activities. It stimulates essential enzymes—a protein kinase and an oligoadenylate synthetase—contributing to the intricate molecular response that fortifies the host's immune defenses against viral threats. Animal-Free IFN-alpha 1a/IFNA1 Protein, Human (His) is the recombinant human-derived animal-FreeIFN-alpha 1a/IFNA1 protein, expressed by E. coli , with N-His labeled tag. The total length of Animal-Free IFN-alpha 1a/IFNA1 Protein, Human (His) is 166 a.a., with molecular weight of ~20.19 kDa.
The CHRNA1 Protein undergoes a substantial conformational shift upon acetylcholine binding, influencing all subunits and leading to the activation of an ion-conducting channel. Yet, the acetylcholine receptor alpha subunit of CHRNA1 can be non-functional in certain cases, underscoring the need to comprehend the factors governing its functionality and integration into fully operational acetylcholine-gated cation-selective channels. CHRNA1 Protein, Human (His) is the recombinant human-derived CHRNA1 protein, expressed by E. coli , with N-6*His labeled tag. The total length of CHRNA1 Protein, Human (His) is 235 a.a., with molecular weight of ~31.1 kDa.
The CHRNA1 Protein undergoes a substantial conformational shift upon acetylcholine binding, influencing all subunits and leading to the activation of an ion-conducting channel. Yet, the acetylcholine receptor alpha subunit of CHRNA1 can be non-functional in certain cases, underscoring the need to comprehend the factors governing its functionality and integration into fully operational acetylcholine-gated cation-selective channels. CHRNA1 Protein, Human (His-Trx) is the recombinant human-derived CHRNA1 protein, expressed by E. coli , with N-Trx, N-6*His labeled tag. The total length of CHRNA1 Protein, Human (His-Trx) is 235 a.a., with molecular weight of ~44.1 kDa.
The DEFA1 protein is a multifunctional effector in innate immunity that exhibits antibiotic-like properties against bacteria, fungi, and viruses. It promotes immune defense by activating antigen-presenting cells (APCs) and inhibiting bacterial cell wall synthesis by interacting with lipid II. DEFA1 Protein, Human (GST) is the recombinant human-derived DEFA1 protein, expressed by E. coli , with N-GST labeled tag. The total length of DEFA1 Protein, Human (GST) is 94 a.a., with molecular weight of ~34 kDa.
CD42b/GP1BA protein is an important platelet membrane protein that interacts with the A1 domain of von Willebrand factor and contributes to the formation of subendothelial platelet plugs. Its GP1BA subunit forms a disulfide-linked complex with two GP1BB subunits, collectively called GP-Ib. CD42b/GP1BA Protein, Human (515a.a, HEK293, His) is the recombinant human-derived CD42b/GP1BA protein, expressed by HEK293 , with C-His labeled tag. The total length of CD42b/GP1BA Protein, Human (515a.a, HEK293, His) is 515 a.a., with molecular weight of 100-130 kDa.
ST6GAL1, a pivotal enzyme, facilitates glycosylation by transferring sialic acid from CMP-sialic acid to galactose-containing acceptor substrates. ST6GAL1 Protein, Human (HEK293, His) is the recombinant human-derived ST6GAL1 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of ST6GAL1 Protein, Human (HEK293, His) is 380 a.a., with molecular weight of 41-60 kDa.
The SDF-1 alpha/CXCL12 protein is a chemoattractant for immune cells. SDF-1 alpha/CXCL12 Protein, Human is the recombinant human-derived SDF-1 alpha/CXCL12 protein, expressed by E. coli , with tag free. The total length of SDF-1 alpha/CXCL12 Protein, Human is 68 a.a., with molecular weight of 8-10.0 kDa.
6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion–transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer[1].
Phenylephrine-2,4,6-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Phenylephrine-d3 (hydrochloride) is the deuterium labeled Phenylephrine hydrochloride. (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
(S)-Phenylephrine-d6 (hydrochloride) is deuterium labeled Phenylephrine (hydrochloride). (R)-(-)-Phenylephrine hydrochloride is a selective α1-adrenoceptor agonist with pKis of 5.86, 4.87 and 4.70 for α1D, α1B and α1A receptors respectively.
Naftopidil-d5 is deuterium labeled Naftopidil. Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia[1][2].
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
Brexpiprazole-d8-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].
RPS6KA3; ISPK1; MAPKAPK1B; RSK2; Ribosomal protein S6 kinase alpha-3; S6K-alpha-3; 90 kDa ribosomal protein S6 kinase 3; p90-RSK 3; p90RSK3; Insulin-stimulated protein kinase 1; ISPK-1; MAP kinase-activated protein kinase 1B; MAPK-activated
WB, IP
Human, Mouse, Rat
Phospho-RSK2 (Ser227) Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 84 kDa, targeting to Phospho-RSK2 (Ser227). It can be used for WB,IP assays with tag free, in the background of Human, Mouse, Rat.
TNF Receptor 2 Antibody is a non-conjugated and Rabbit origined polyclonal antibody about 48 kDa, targeting to TNF Receptor 2. It can be used for WB,IHC-F,IHC-P,ICC/IF,FC,IP assays with tag free, in the background of Human, Mouse, Rat.
CD79a Antibody is a non-conjugated and Rabbit origined monoclonal antibody about 25 kDa, targeting to CD79a. It can be used for WB,IHC-F,IHC-P,ICC/IF assays with tag free, in the background of Human.
Autophagy related protein LC3 A; Autophagy related protein LC3 B; Autophagy related ubiquitin like modifier LC3 A; Autophagy related ubiquitin like modifier LC3 B; MAP1 light chain 3 like protein 1; MAP1 light chain 3 like protein 2; MAP1A/1B light chain 3 A; MAP1A/1B light chain 3 B; MAP1A/1BLC3; MAP1A/MAP1B LC3 A; MAP1A/MAP1B LC3 B; MAP1ALC3; MAP1BLC3; MAP1LC3A; MAP1LC3B; Microtubule associated protein 1 light chain 3 alpha; Microtubule associated protein 1 light chain 3 beta; Microtubule associated proteins 1A/1B light chain 3; Microtubule associated proteins 1A/1B light chain 3A; Microtubule associated proteins 1A/1B light chain 3B; MLP3A_HUMAN.
WB, ELISA, IHC-P, IHC-F, FC, ICC/IF
Human, Rat
LC3 Antibody is an unconjugated, approximately 14/16 kDa, rabbit-derived, anti-LC3 polyclonal antibody. LC3 Antibody can be used for: WB, ELISA, IHC-P, IHC-F, Flow-Cyt, IF expriments in human, rat, and predicted: mouse, chicken, dog, pig, cow, horse, sheep, goat background without labeling.
Caspase-1 p20 Antibody is an unconjugated, approximately 20/46 kDa, rabbit-derived, anti-Caspase-1 p20 polyclonal antibody. Caspase-1 p20 Antibody can be used for: WB, ELISA, IHC-P, IHC-F, Flow-Cyt, ICC, IF expriments in human, mouse, rat, background without labeling.
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