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unbound

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Androgen Receptor (1) Casein Kinase (1) Cytochrome P450 (1) Endogenous Metabolite (2) Fluorescent Dye (2)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Infection (1) Metabolic Disease (1)

Inhibitors & Agonists

Fluorescent Dye

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-117789

Keto-itraconazole keto-ITZ	Cytochrome P450	Infection Cancer
Keto-itraconazole (keto-ITZ) is a metabolism of Itraconazole (HY-17514) with a potent inhibitor activity of CYP3A. Keto-itraconazole shows unbound IC₅₀ value of 4.6 nM when coincubated with human liver microsomes and midazolam .

HY-110250

DFHBI 5+ Cited Publications	Fluorescent Dye	Others
DFHBI is a small molecule that resembles the chromophore of green fluorescent protein (GFP). DFHBI can be used for imaging RNA in living cells. . Spinach and DFHBI are essentially nonfluorescent when unbound, whereas the Spinach-DFHBI complex is brightly fluorescent both in vitro and in living cells (Ex/Em = 469/501 nm).

HY-E70408

12α-Hydroxysteroid dehydrogenase, bacillus sphaericus	Endogenous Metabolite	Metabolic Disease
12α-Hydroxysteroid dehydrogenase, bacillus sphaericus is a dehydrogenase expressed in Bacillus sphaericus. 12α-Hydroxysteroid dehydrogenase, bacillus sphaericus is NAD-dependent and is active on both bound and unbound bile salts. This enzyme can be used to measure the concentration of 12α-hydroxy bile acids in serum .

HY-D0121B

INDO 1 pentasodium	Fluorescent Dye	Others
INDO 1 pentasodium is a ratiometric, free calcium ion (Ca ²⁺) fluorescent indicator that can quantitatively monitor dynamic changes in intracellular free Ca ²⁺ concentrations. When unbound to Ca ²⁺ (free state), INDO 1 pentasodium exhibits a peak emission wavelength of 485 nm under UV excitation (350 nm). Upon binding to Ca ²⁺ (bound state), the emission peak shifts to 405 nm. INDO 1 pentasodium is highly photolabile and susceptible to photobleaching, and its emission spectrum may overlap with the autofluorescence of NADH .

HY-135541

Darexaban maleate YM150 maleate	Endogenous Metabolite	Cardiovascular Disease
Darexaban maleate (YM150 maleate) is a direct factor Xa inhibitor with activity in preventing venous thromboembolism. The major metabolite of Darexaban maleate in humans is Darexaban glucitol, which acts pharmacologically. The glucitolation reaction of Darexaban maleate is mainly catalyzed by UGT1A9 and UGT1A10 in the human liver and intestine. The K(m) value of Darexaban maleate glucitolation in the liver is greater than 250 μM, while in the intestine it exhibits substrate inhibition kinetics with a K(m) value of 27.3 μM. The unbound K(m) value of Darexaban maleate is significantly reduced by the influence of fatty acid-free bovine serum albumin in both HLM and UGT1A9 .

HY-403733A

(–)-JJ-450	Androgen Receptor	Cancer
(-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR ^F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .

HY-178980

APL-5125	Casein Kinase	Cancer
APL-5125 (Compound 61f) is a potent, selective and orally active ATP-competitive CK2α inhibitor with an IC₅₀ of 0.348 nM and a K_i of 0.095 nM. APL-5125 binds to CK2α in a bivalent manner, simultaneously interacting with the ATP-binding site and the αD pocket. APL-5125 exhibits antitumor activity and can be used for the research of cancer, such as colon cancer .

Cat. No.	Product Name	Type

HY-110250

DFHBI 5+ Cited Publications	Fluorescent Dyes/Probes
DFHBI is a small molecule that resembles the chromophore of green fluorescent protein (GFP). DFHBI can be used for imaging RNA in living cells. . Spinach and DFHBI are essentially nonfluorescent when unbound, whereas the Spinach-DFHBI complex is brightly fluorescent both in vitro and in living cells (Ex/Em = 469/501 nm).

HY-D0121B

INDO 1 pentasodium	Fluorescent Dyes/Probes
INDO 1 pentasodium is a ratiometric, free calcium ion (Ca ²⁺) fluorescent indicator that can quantitatively monitor dynamic changes in intracellular free Ca ²⁺ concentrations. When unbound to Ca ²⁺ (free state), INDO 1 pentasodium exhibits a peak emission wavelength of 485 nm under UV excitation (350 nm). Upon binding to Ca ²⁺ (bound state), the emission peak shifts to 405 nm. INDO 1 pentasodium is highly photolabile and susceptible to photobleaching, and its emission spectrum may overlap with the autofluorescence of NADH .

INDO 1 pentasodium

Fluorescent Dyes/Probes

INDO 1 pentasodium is a ratiometric, free calcium ion (Ca ²⁺) fluorescent indicator that can quantitatively monitor dynamic changes in intracellular free Ca ²⁺ concentrations. When unbound to Ca ²⁺ (free state), INDO 1 pentasodium exhibits a peak emission wavelength of 485 nm under UV excitation (350 nm). Upon binding to Ca ²⁺ (bound state), the emission peak shifts to 405 nm. INDO 1 pentasodium is highly photolabile and susceptible to photobleaching, and its emission spectrum may overlap with the autofluorescence of NADH .

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