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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
257 Results for "
concentration-dependent
" in MedChemExpress (MCE) Product Catalog:
Products (257)
257 Results for "concentration-dependent" in MCE Product Catalog:
Cat. No.: HY-113252S1
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2-Methoxyestrone- 13C6 is the 13C-labeled 2-Methoxyestrone (HY-113252). 2-Methoxyestrone is an estrogen metabolite with antimitotic activity. 2-Methoxyestrone acts as a liver-specific prohormone that undergoes demethylation to form active 2-hydroxyestrogens, and it can also interconvert with 2-Methoxyestradiol (HY-12033) via the 17β-hydroxysteroid dehydrogenase pathway. In the presence of all-trans retinoic acid, 2-Methoxyestrone exerts a strong, concentration-dependent inhibitory effect on cell growth. 2-Methoxyestrone delays the progression of pulmonary hypertension in rats, alleviates right ventricular and pulmonary vascular remodeling, and relieves proliferative pulmonary hypertension in rats. 2-Methoxyestrone can be used in studies related to proliferative pulmonary hypertension .
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2-Methoxyestrone-d4 is the deuterated-labeled 2-Methoxyestrone (HY-113252). 2-Methoxyestrone is an estrogen metabolite with antimitotic activity. 2-Methoxyestrone acts as a liver-specific prohormone that undergoes demethylation to form active 2-hydroxyestrogens, and it can also interconvert with 2-Methoxyestradiol (HY-12033) via the 17β-hydroxysteroid dehydrogenase pathway. In the presence of all-trans retinoic acid, 2-Methoxyestrone exerts a strong, concentration-dependent inhibitory effect on cell growth. 2-Methoxyestrone delays the progression of pulmonary hypertension in rats, alleviates right ventricular and pulmonary vascular remodeling, and relieves proliferative pulmonary hypertension in rats. 2-Methoxyestrone can be used in studies related to proliferative pulmonary hypertension .
Cat. No.: HY-147412D
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FAM labled Ultevursen sodiumis a FAM labled Ultevursen sodium (HY-147412A). Ultevursen sodium (QR-421a) is a splice-modulating antisense oligonucleotide targeting exon 13 of the USH2A gene, which restores the functional expression of Usherin protein by inducing exon skipping. Ultevursen sodium binds to USH2A pre-mRNA and modulates the splicing process to specifically skip exon 13 carrying the pathogenic mutation c.2299delG, generating an in-frame transcript and a truncated yet functionally normal protein. Ultevursen sodium exhibits concentration-dependent exon skipping activity in human cells and retinal organoid models, and restores Usherin expression and retinal function in zebrafish and gene-edited mouse models. Ultevursen sodium can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa .
Cat. No.: HY-147412E
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Cy3 labled Ultevursen sodium is a Cy3 labled Ultevursen sodium (HY-147412A). Ultevursen sodium (QR-421a) is a splice-modulating antisense oligonucleotide targeting exon 13 of the USH2A gene, which restores the functional expression of Usherin protein by inducing exon skipping. Ultevursen sodium binds to USH2A pre-mRNA and modulates the splicing process to specifically skip exon 13 carrying the pathogenic mutation c.2299delG, generating an in-frame transcript and a truncated yet functionally normal protein. Ultevursen sodium exhibits concentration-dependent exon skipping activity in human cells and retinal organoid models, and restores Usherin expression and retinal function in zebrafish and gene-edited mouse models. Ultevursen sodium can be used for related research on type 2 Usher syndrome and non-syndromic retinitis pigmentosa .
Cat. No.: HY-179038
CAS No.: 433702-41-1
PYO12 is a 3-phenyl-4-phenoxypyrazole type antibacterial compound. PYO12 exhibits selective activity against Gram-positive bacteria with MIC for S. aureus, B. subtilis, S. pneumoniae, and MRSA of 1, 1, 1, and 4 μg/mL respectively. PYO12 has no activity against Gram-negative bacteria. PYO12 can significantly increase bacterial membrane permeability and significantly upregulate cell wall stress-related genes, possibly by binding to the C55-PP part of lipid II. PYO12 shows a concentration-dependent bactericidal effect, has low toxicity to mammalian cells, and does not cause hemolysis. PYO12 can be used to develop new antibiotics targeting bacterial cell wall synthesis .
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Parethoxycaine (Intracaine) is an ester-type local anesthetic that possesses dual activities as a non-selective inhibitor and agonist potentiator in smooth muscle, while acting as a mixed-type inhibitor of cytochrome c oxidase at the enzyme level. Parethoxycaine non-competitively inhibits the contraction of guinea pig ileal longitudinal muscle by interfering with transmembrane Ca 2+ transport (blocking K +/CD responses in an equi-effective manner), and potentiates norepinephrine (NA) responses in rat vas deferens by blocking NA uptake and promoting Ca 2+ mobilization (increasing the maximum amplitude without affecting K + responses). Parethoxycaine inhibits the activity of purified cytochrome c oxidase in a concentration-dependent manner, and can be used in research focusing on Ca 2+ signal transduction, smooth muscle contraction regulation, and mitochondrial energy metabolism .
Cat. No.: HY-B1777S
CAS No.: 93827-50-0
Synonyms: NSC 268508-15N2; Neuridine-15N2
Cat. No.: HY-Y1890B
CAS No.: 61791-12-6
Cat. No.: HY-153164
CAS No.: 879054-55-4
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VU0606170 is a selective Slack channel inhibitor with low micromolar potency. VU0606170 can reduce the frequency of neuronal Calcium oscillations in a concentration dependent manner. VU0606170 can be used for research on diseases such as epilepsy .
Cat. No.: HY-101460R
CAS No.: 2087490-42-2
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Tz-Thalidomide (Standard) is the analytical standard of Tz-Thalidomide (HY-101460). This product is intended for research and analytical applications. Tz-Thalidomide is a tetrazine-tagged Thalidomide (HY-14658), an E3 ligase ligand. Tz-Thalidomide self-assembles with TCO-labeled target protein inhibitors, forming a CLIP-TAC (targeted protein degradation chimera) via click chemistry. This chimera recruits the E3 ubiquitin ligase CRBN to the target protein, thereby inducing ubiquitination and subsequent degradation of the target protein. When used in combination with JQ1-TCO (HY-148864), Tz-Thalidomide induces concentration-dependent degradation of BRD4 in cells. When combined with ERK-targeting protein inhibitors, Tz-Thalidomide induces degradation of ERK1/2 in cells. Tz-Thalidomide can be used in cancer-related research .
Cat. No.: HY-137325A
CAS No.: 301334-89-4
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2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
Cat. No.: HY-172085
CAS No.: 3099543-90-2
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SH514 is an orally active IRF4 inhibitor (IC50 = 2.63 μM). SH514 binds to the IRF4-DBD domain, thereby inhibiting the interaction of IRF4 protein with DNA (KD = 1.28 μM). SH514 can inhibit the proliferation of IRF4-high-expressing NCI-H929 and MM.1R cells, and displays no cytotoxicity for normal cells. SH514 significantly downregulates the expression of IRF4 downstream target genes concentration-dependently. SH514 inhibits the expression of cell cycle-related proteins CDC2, Cyclin B1, Cyclin D1, Cyclin E1, and CMYC in Multiple Myeloma cells. SH514 can induce DNA damage and increase the expression of γH2AX. SH514 effectively inhibits the proliferation of multiple myeloma tumors .
Cat. No.: HY-178020
CAS No.: 3020729-11-4
FLT3-IN-34 is a FLT3 inhibitor, with an IC50 value of 1.4 nM. FLT3-IN-34 blocks the phosphorylation of FLT3 and its downstream signaling molecules AKT and ERK1/2. FLT3-IN-34 induces concentration-dependent G0/G1 phase arrest and mild apoptosis in FLT3-ITD-positive MV4-11 cells. FLT3-IN-34 shows potent anti-proliferative activity against FLT3-ITD-positive MV4-11 cells (IC50 = 14.95 nM) and MOLM-13 (IC50 = 18.5 nM). FLT3-IN-34 can be used for the study of FLT3-positive acute myeloid leukemia (AML) .
Cat. No.: HY-N0245R
CAS No.: 30462-34-1
Cat. No.: HY-W338810S
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S-(5'-Adenosyl)-L-methionine- 13C5 sulfate is the 13C-labeled S-(5'-Adenosyl)-L-methionine chloride (HY-W338810). S-(5'-Adenosyl)-L-methionine chloride is the endogenous methyl donor in the methionine cycle and numerous methylation reactions, including protein methylation. S-(5'-Adenosyl)-L-methionine chloride can activate cardiac ryanodine receptor RyR2 in a concentration-dependent manner, enhancing the affinity of RyR2 for ryanodine. The Kd of S-(5'-Adenosyl)-L-methionine chloride with MetJ in Escherichia coli is 0.18 mM. S-(5'-Adenosyl)-L-methionine chloride can cause changes in the methylation index of Cisplatin (HY-17394)-sensitive and Cisplatin-resistant ovarian cancer cells. S-(5'-Adenosyl)-L-methionine chloride can be used for methylation-related research .
Cat. No.: HY-P5493
CAS No.: 103412-42-6
Synonyms: B-3824 free base
D-Arg-[Hyp3,Thi5,8,D-Phe7]-Bradykinin is a biological active peptide. (inhibited bradykinin-induced contractions concentration dependently; bradykinin B2 receptor antagonist)
Synonyms: MK-678; L-363586
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Chlorpromazine (Standard) is the analytical standard of Chlorpromazine (HY-12708). This product is intended for research and analytical applications. Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis .
Cat. No.: HY-138074
CAS No.: 93074-04-5
Synonyms: 5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime
Milbemycin A4 oxime (5-Ketomilbemycin A4 oxime; 5-Oxomilbemycin A4 5-oxime) is a derivative of Milbemycin A4 (HY-126906) and a component of Milbemycin oxime (HY-B0778), both of which have insecticidal and nematicidal activities. Milbemycin A4 oxime (0.05 mg/kg) reduces the number of microfilariae in naturally infected dogs with D. immitis and inhibits the growth of clinical isolates of Candida glabrata (MIC80=16-32 μg/mL). Milbemycin A4 oxime (2.5 μg/mL) blocks the efflux of Fluconazole (HY-B0101) from clinical isolates of Candida glabrata. Milbemycin A4 oxime enhances doxorubicin-induced cell growth inhibition and increases the intracellular accumulation of doxorubicin and P-glycoprotein substrate Rhodamine 123 (HY-D0816) in doxorubicin-resistant but not sensitive MCF-7 breast cancer cells in a concentration-dependent manner.
Cat. No.: HY-156807
CAS No.: 210751-39-6
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LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .
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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
