Synthesis, characterization, alkaline phosphatase inhibition assay and molecular modeling studies of 1-benzylidene-2-(4-tert- butylthiazol-2-yl) hydrazines

Synthesis, characterization, alkaline phosphatase inhibition assay and molecular modeling studies of 1-benzylidene-2-(4-tert- butylthiazol-2-yl) hydrazines

alkaline phosphatase is an enzyme that removes phosphate homodimeric proteins of several types of molecules. This catalyzes the hydrolysis of monoesters in phosphoric acid, which in turn catalyzes transfosforilasi. Thiazoles is a special class of heterocyclic compounds that could potentially be an effective phosphatase inhibitors. In this case, this research paper reported the synthesis and characterization smoothly substituted 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine with excellent results.

Synthesized compounds tested for potency inhibition of alkaline phosphatase. The compound 1- (4-hydroxy, 3-methoxybenzylidene) -2- (4-tert-butylthiazol-2-yl) hydrazine (<b> 5e) </ b> was found to be the most potent inhibitor of human tissue non phosphatase -alkaline in this group of molecules with IC <sub> 50 </ sub> value of 1.09 ± 0.18 pM. The compound 1- (3,4-dimethoxybenzylidene) -2- (4-tert-butylthiazol-2-yl) hydrazine <b> (5d) </ b> exhibited selectivity and the potential for human intestinal alkaline phosphatase with IC <sub> 50 </ sub> value of 0.71 ± 0.02 pM.

In addition, the structure activity relationship and molecular docking studies were performed to evaluate their mode of binding to the target site alkaline phosphatase. Docking analysis revealed that the most active inhibitor showed significant interaction in the binding pocket of human intestinal alkaline phosphatase and alkaline phosphatase non-human tissues and may be responsible for the inhibitory activity of compounds against the enzyme. Therefore, the filtered thiazole derivatives provided a superb platform for the further development of alkaline phosphatase inhibitor.

Alkaline phosphatase assay revealed the compound <b> 5e </ b> (1- (4-hydroxy, 3-methoxybenzylidene) -2- (4-tert-butylthiazol-2-yl) hydrazine) as the most active inhibitor <b> < i> h </ i> -TNAP </ b> IC <sub> 50 </ sub> value of 1.09 ± 0.18 pM. Computing evaluation clearly illustrates the multiple interactions in the binding pocket <b> <i> h </ i> -IAP </ b> and <b> <i> h </ i> -TNAP </ b> and may be responsible for potential inhibitory compounds against the enzyme. Highlights Synthesis of 1- (benzylidene) thiosemicarbazides <b> 3 (a-i) </ b> reacting it with substituted aromatic aldehydes

Thiosemicarbazide <b> 1 (a-i) </ b>. synthesized 1- (benzylidene) thiosemicarbazides was cyclized with 1-chloropinacolone to get each 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine <b> 5 (a-i) </ b>. synthesized 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine <b> 5 (a-i) </ b> successfully characterized using elemental analysis, FT-IR and multi nuclear NMR. Alkaline phosphatase assay and computational studies conducted in support of 1-benzylidene-2- (4-tert-butylthiazol-2-yl) hydrazine synthesized <b> 5 (a-i) </ b>.

Reduce background absorption through the double-key strategy for the detection of alkaline phosphatase and α-fetoprotein

Lowering the background signal for analysis is more sensitive than determinands equally important to strengthen the target signal. Oxidase photoinduced of fluorescein have been reported, which can catalyze the oxidation of a common substrate in a few minutes. As a metaphor for the lock and key, we designed a double lock limiting the activity of fluorescein to reduce background uptake during colorimetric detection.

Genorise® Alkaline Phosphatase Activity Fluorometric Assay Kit

GR107016 100 tests
EUR 289

StemTAG Alkaline Phosphatase Activity Assay Kit, Fluorometric

CBA-307 100 assays
EUR 540
Description: Alkaline Phosphatase (AP) is a widely used marker for both mouse and human embryonic stem cells (ES) and embryonic germ cells (EG). Our StemTAG Alkaline Phosphatase kits provide an efficient system for monitoring cell differentiation or undifferentiation using the AP marker. The StemTAG Alkaline Phosphatase Activity Assay Kits provide reagents for quantifying alkaline phosphatase activity in a convenient 96-well plate format, with either colorimetric or fluorescence detection.

StemTAG Alkaline Phosphatase Staining and Activity Assay Kit, Fluorometric

CBA-308 2 x 100 assays
EUR 846
Description: Alkaline Phosphatase (AP) is a widely used marker for both mouse and human embryonic stem cells (ES) and embryonic germ cells (EG). Our StemTAG Alkaline Phosphatase kits provide an efficient system for monitoring cell differentiation or undifferentiation using the AP marker. The StemTAG Alkaline Phosphatase Activity Assay Combo Kits provide reagents for monitoring alkaline phosphatase activity via immunocytochemistry staining as well as in a 96-well plate with either colorimetric or fluorescence detection.

Acid Phosphatase Activity Fluorometric Assay Kit

K421-500 each
EUR 418.8

Protein Tyrosine Phosphatase Activity Assay Kit (Fluorometric)

K829-100 each
EUR 639.6

Alkaline Phosphatase Activity Assay Kit

55R-1402 500 assays
EUR 888
Description: Assay Kit for detection of Alkaline Phosphatase in the research laboratory

Alkaline Phosphatase Activity Assay Kit

55R-1406 500 assays
EUR 525.6
Description: Assay Kit for detection of Alkaline Phosphatase in the research laboratory

Alkaline Phosphatase Activity Colorimetric Assay Kit

K2075-500 500 assays
EUR 652.8

Alkaline Phosphatase Activity Colorimetric Assay Kit

K412-500 each
EUR 646.8

Phospholipase A2 Activity Assay Kit (Fluorometric)

K400-100 each
EUR 679.2

HAT Activity Fluorometric Assay Kit

K2034-100 100 assays
EUR 668.4

HAT Activity Fluorometric Assay Kit

K334-100 each
EUR 646.8

DPP4 Activity Fluorometric Assay Kit

K779-100 each
EUR 652.8

HDAC Activity Fluorometric Assay Kit

K2031-100 100 assays
EUR 602.4

PLTP Activity Fluorometric Assay Kit

K2087-100 100 assays
EUR 802.8

CETP Activity Fluorometric Assay Kit

K2089-100 100 assays
EUR 870

DPP4 Activity Fluorometric Assay Kit

K2178-100 100 assays
EUR 668.4

HDAC Activity Fluorometric Assay Kit

K330-100 each
EUR 588

HDAC Activity Fluorometric Assay Kit

K2031-96 96 tests
EUR 486
Description: Detects HDAC activity, high throughput screening (HTS).

Renin Activity Fluorometric Assay Kit

K800-100 each
EUR 627.6

HDAC3 Activity Fluorometric Assay Kit

K343-100 each
EUR 574.8

HDAC8 Activity Fluorometric Assay Kit

K348-100 each
EUR 588

StemTAG Alkaline Phosphatase Activity Assay Kit, Colorimetric

CBA-301 100 assays
EUR 483.6
Description: Alkaline Phosphatase (AP) is a widely used marker for both mouse and human embryonic stem cells (ES) and embryonic germ cells (EG). Our StemTAG Alkaline Phosphatase kits provide an efficient system for monitoring cell differentiation or undifferentiation using the AP marker. The StemTAG Alkaline Phosphatase Activity Assay Kits provide reagents for quantifying alkaline phosphatase activity in a convenient 96-well plate format, with either colorimetric or fluorescence detection.

Calpain Activity Fluorometric Assay Kit

K2062-100 100 assays
EUR 752.4

Calpain Activity Fluorometric Assay Kit

K240-100 each
EUR 705.6

Protease Activity Fluorometric Assay Kit

K781-100 each
EUR 464.4

Thrombin Activity Fluorometric Assay Kit

K373-100 each
EUR 836.4

HAT (H4) Activity Fluorometric Assay Kit

K336-100 each
EUR 601.2

Alkaline Phosphatase Activity Assay Catalog: MA-0109

MA-0109 100 wells
EUR 475

Urokinase Activity Fluorometric Assay Kit

K728-100 each
EUR 652.8

Alkaline Phosphatase Colorimetric Activity Kit (2 Plate)

K082-H1 2x96 well plate
EUR 289

MMP-3 Activity Fluorometric Assay Kit

K783-100 each
EUR 614.4

PLTP Activity Fluorometric Assay Kit II

K593-100 each
EUR 705.6

CETP Activity Fluorometric Assay Kit II

K595-100 each
EUR 770.4

Proteasome Activity Fluorometric Assay Kit

K2096-100 100 assays
EUR 602.4

Proteasome Activity Fluorometric Assay Kit

K245-100 each
EUR 574.8

Total Phosphodiesterase Activity Assay Kit (Fluorometric)

K927-100 each
EUR 738

Genorise® Alkaline Phosphatase Activity Colorimetric Assay Kit

GR107015 100 tests
EUR 289

Rat Renin Activity Fluorometric Assay Kit

K806-100 each
EUR 777.6

Factor Xa Activity Fluorometric Assay Kit

K361-100 each
EUR 744

Lipase Activity Fluorometric Assay Kit III

K724-100 each
EUR 639.6

Lipase Activity Fluorometric Assay Kit III

K2095-100 100 assays
EUR 703.2

Caspae-9 Activity Fluorometric Assay Kit

RP10239K 1kit
EUR 552.5

Neuraminidase Activity Fluorometric Assay Kit

K732-100 each
EUR 627.6

Neuraminidase Activity Fluorometric Assay Kit

K2230-100 100 assays
EUR 718.8

GST Fluorometric Activity Assay Kit

K260-100 each
EUR 561.6

GST Fluorometric Activity Assay Kit

K2105-100 100 assays
EUR 602.4

Granzyme B Activity Fluorometric Assay Kit

K168-100 each
EUR 639.6

Granzyme B Activity Fluorometric Assay Kit

K2001-100 100 assays
EUR 703.2

InSitu HDAC Activity Fluorometric Assay Kit

K339-100 each
EUR 574.8

Cathepsin H Activity Fluorometric Assay Kit

K145-100 each
EUR 574.8

Cathepsin L Activity Fluorometric Assay Kit

K142-100 each
EUR 614.4

Cathepsin D Activity Fluorometric Assay Kit

K143-100 each
EUR 614.4

Cathepsin S Activity Fluorometric Assay Kit

K144-100 each
EUR 614.4

Cathepsin B Activity Fluorometric Assay Kit

K140-100 each
EUR 614.4

Cathepsin K Activity Fluorometric Assay Kit

K141-100 each
EUR 614.4

Cathepsin B Activity Fluorometric Assay Kit

K2151-100 100 assays
EUR 619.2

Cathepsin K Activity Fluorometric Assay Kit

K2152-100 100 assays
EUR 619.2

Cathepsin L Activity Fluorometric Assay Kit

K2153-100 100 assays
EUR 619.2

Cathepsin D Activity Fluorometric Assay Kit

K2154-100 100 assays
EUR 619.2

Cathepsin S Activity Fluorometric Assay Kit

K2155-100 100 assays
EUR 619.2

Proteasome Activity Fluorometric Assay Kit I

RP10220K 1Kit
EUR 455

Proteasome Activity Fluorometric Assay Kit II

RP10221K 1Kit
EUR 650

HDAC6 Activity Assay Kit (Fluorometric)

K466-100 each
EUR 757.2

Sphingomyelinase Activity Fluorometric Assay Kit

K574-100 each
EUR 548.4

GST Fluorometric Activity Assay

KT-205 100 tests
EUR 510

Uricase Activity Assay Kit (Fluorometric)

K734-100 each
EUR 614.4

Plasmin Activity Assay Kit (Fluorometric)

K381-100 each
EUR 548.4

Sirtuin Activity Assay Kit (Fluorometric)

K324-100 each
EUR 686.4

PPDK (Pyruvate, phosphate dikinase) Activity Assay Kit (Fluorometric/Colorimetric)

K456-100 each
EUR 574.8

Beta-Secretase Activity Fluorometric Assay Kit

K2043-100 100 assays
EUR 769.2

Beta-Secretase Activity Fluorometric Assay Kit

K360-100 each
EUR 744

Caspase-8, 10 Activity Fluorometric Assay Kit

RP10238K 1kit
EUR 552.5

Caspase-3, 7 Activity Fluorometric Assay Kit

RP10240K 1kit
EUR 552.5

Lysozyme Activity Assay Kit (Fluorometric)

K236-100 each
EUR 588

Purine Nucleoside Phosphorylase Activity Assay Kit (Fluorometric)

K767-100 each
EUR 914.4

Lipoprotein Lipase Activity Fluorometric Assay Kit

K721-100 each
EUR 646.8

DNAse I Activity Assay Kit (Fluorometric)

K429-100 each
EUR 836.4

?-Xylosidase Activity Assay Kit (Fluorometric)

K981-100 each
EUR 705.6

Neprilysin Activity Assay Kit (Fluorometric)

K487-100 each
EUR 732

Lipoxygenase Activity Assay Kit (Fluorometric)

K978-100 each
EUR 783.6

Chymotrypsin Activity Assay Kit (Fluorometric)

K352-100 each
EUR 588

Factor IXa Activity Assay Kit (Fluorometric)

K364-100 each
EUR 588

?-Glucuronidase Activity Assay Kit (Fluorometric)

K514-100 each
EUR 744

Deubiquitinase Activity Assay Kit (Fluorometric)

K485-100 each
EUR 639.6

StemTAG Alkaline Phosphatase Staining and Activity Assay Kit, Colorimetric

CBA-302 2 x 100 assays
EUR 769.2
Description: Alkaline Phosphatase (AP) is a widely used marker for both mouse and human embryonic stem cells (ES) and embryonic germ cells (EG). Our StemTAG Alkaline Phosphatase kits provide an efficient system for monitoring cell differentiation or undifferentiation using the AP marker. The StemTAG Alkaline Phosphatase Activity Assay Combo Kits provide reagents for monitoring alkaline phosphatase activity via immunocytochemistry staining as well as in a 96-well plate with either colorimetric or fluorescence detection.

TEV Protease Activity Assay Kit (Fluorometric)

K842-100 each
EUR 601.2

Cathepsin E Activity Assay Kit (Fluorometric)

K165-100 each
EUR 764.4

Factor VIIIa Activity Assay Kit (Fluorometric)

K358-100 each
EUR 646.8

Chitotriosidase Activity Assay Kit (Fluorometric)

K512-100 each
EUR 744

Lysyl Oxidase Activity Assay Kit (Fluorometric)

K928-100 each
EUR 639.6

Enolase Activity Colorimetric/Fluorometric Assay Kit

K691-100 each
EUR 952.8

?-L-Fucosidase Activity Assay Kit (Fluorometric)

K542-100 each
EUR 627.6

Methyltransferase Activity Assay Kit (Fluorometric)

K521-100 each
EUR 679.2

Adenosylhomocysteinase (AHCY) Activity Fluorometric Assay Kit

K807-100 each
EUR 1038

Enteropeptidase/Enterokinase Activity Fluorometric Assay Kit

K758-100 each
EUR 732

Catalase Activity Colorimetric/Fluorometric Assay Kit

K773-100 each
EUR 502.8

Catalase Activity Colorimetric/Fluorometric Assay Kit

K2177-100 100 assays
EUR 501.6

Oxalate Oxidase Activity Assay Kit (Fluorometric)

K509-100 each
EUR 574.8

Diamine Oxidase Activity Assay Kit (Fluorometric)

K496-100 each
EUR 679.2

?-Secretase (BACE1) Activity Assay Kit (Fluorometric)

K388-100 each
EUR 724.8

Caspase-3 Activity Assay Kit II (Fluorometric)

K533-100 each
EUR 614.4

Aromatase (CYP19A) Activity Assay Kit (Fluorometric)

K983-100 each
EUR 744

Peroxidase Activity Colorimetric/Fluorometric Assay Kit

K772-100 each
EUR 464.4

Pepsin/Pepsinogen Activity Assay Kit (Fluorometric)

K446-100 each
EUR 561.6

HIV-1 Protease Activity Assay Kit (Fluorometric)

K825-100 each
EUR 679.2

HIV-2 Protease Activity Assay Kit (Fluorometric)

K845-100 each
EUR 705.6

Cytidine Deaminase Activity Assay Kit (Fluorometric)

K451-100 each
EUR 561.6

Cyclooxygenase (COX) Activity Assay Kit (Fluorometric)

K549-100 each
EUR 502.8

Beta-Mannosidase Activity Assay Kit (Fluorometric)

K2045-100 100 assays
EUR 661.2

OxiSelect Catalase Activity Assay Kit, Fluorometric

STA-339 500 assays
EUR 908.4
Description: Catalase is a ubiquitous enzyme that destroys hydrogen peroxides formed during oxidative stress. Our OxiSelect Catalase Activity Assay Kit measures catalase activity in less than one hour from a variety of samples including blood, cells and tissues. Each kit provides sufficient reagents to perform up to 500 assays in a 96-well microtiter plate. This includes blanks, catalase standards and unknown samples. The OxiSelect Catalase Activity Assay Kit (Fluorometric) provides a 40-fold increase in sensitivity compared to our colorimetric assay.

Asparaginase Activity Colorimetric/Fluorometric Assay Kit

K754-100 each
EUR 660

Myeloperoxidase (MPO) Fluorometric Activity Assay Kit

K745-100 each
EUR 660

Neutrophil Elastase Activity Assay kit (Fluorometric)

K383-100 each
EUR 502.8

Myeloperoxidase (MPO) Fluorometric Activity Assay Kit

K2169-100 100 assays
EUR 686.4

Adenosine Deaminase Activity Assay Kit (Fluorometric)

K328-100 each
EUR 548.4

PicoProbe? Hexokinase Activity Assay Kit (Fluorometric)

K769-100 each
EUR 764.4

Paraoxonase 1 (PON1) Activity Assay Kit (Fluorometric)

K999-100 each
EUR 744

Choline Kinase (ChoK) Activity Assay Kit (Fluorometric)

K476-100 each
EUR 1136.4

PicoProbe? 15-PGDH Activity Assay Kit (Fluorometric)

K562-100 each
EUR 639.6

Gamma Glutamyl Transferase (GGT) Activity Fluorometric Assay Kit

K785-100 each
EUR 588

PicoProbe? Aldehyde Dehydrogenase Activity Fluorometric Assay Kit

K741-100 each
EUR 686.4

CheKine™ Micro Tissue and Blood Alkaline Phosphatase (AKP/ALP) Activity Assay Kit

KTB1700-48T 48 T
EUR 29
Description: Abbkine CheKine™ Tissue and Blood Alkaline Phosphatase(AKP/ALP)Colorimetric Assay Kit is designed for detecting Alkaline Phosphatase activity in the sample.

CheKine™ Micro Tissue and Blood Alkaline Phosphatase (AKP/ALP) Activity Assay Kit

KTB1700-96T 96 T
EUR 49
Description: Abbkine CheKine™ Tissue and Blood Alkaline Phosphatase(AKP/ALP)Colorimetric Assay Kit is designed for detecting Alkaline Phosphatase activity in the sample.

Cystathionine ? Synthase Activity Assay Kit (Fluorometric)

K998-100 each
EUR 744

PicoProbeTM Glucokinase Activity Assay Kit (Fluorometric)

K969-100 each
EUR 711.6

Glucose Oxidase Activity Colorimetric/Fluorometric Assay Kit

K788-100 each
EUR 646.8

Pyruvate Kinase Activity Colorimetric/Fluorometric Assay Kit

K709-100 each
EUR 732

Xanthine Oxidase Activity Colorimetric/Fluorometric Assay Kit

K710-100 each
EUR 489.6

Pyruvate Kinase Activity Colorimetric/Fluorometric Assay Kit

K2223-100 100 assays
EUR 752.4

Xanthine Oxidase Activity Colorimetric/Fluorometric Assay Kit

K2224-100 100 assays
EUR 501.6

Beta Galactosidase (?-Gal) Activity Assay Kit (Fluorometric)

K821-100 each
EUR 601.2

Lipoprotein Lipase (LPL) Activity Assay Kit (Fluorometric)

STA-610 100 assays
EUR 644.4
Description: The Lipoprotein Lipase (LPL) Activity Assay Kit is a simple, fluorometric assay that quantitatively measures LPL activity in plasma, serum, and lysates in a 96-well microtiter plate format.  Each kit provides sufficient reagents to perform up to 100 assays, including blanks, LPL standards, and unknown samples.  The kit contains a LPL Standard and has a detection sensitivity limit of ~1 mUnits/mL (see Kit Components for unit definition). Besides LPL, this assay can also be used to detect endothelial and hepatic lipase activity.

EpiQuik HDAC Activity/Inhibition Assay Kit (Fluorometric)

P-4001 96 Assays
EUR 684.66

The first key inhibit the main activity of fluorescein by phosphate. The second key is almost completely disable fluorescein by forming nanoparticles coordination (CNPS) through self-assembly of cerium chloride and fluorescein diphosphate (FDP).