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Ethidium homodimer (EthD-1) is a high-affinity fluorescent nucleic acid dye commonly used to stain mammals, bacteria, yeast, and fungi. Ethidium homodimer binds to DNA or RNA, enhancing fluorescence more than 30 times. The Ethidium homodimer has a strong positive charge, so it cannot cross cell membranes and stain living cells; But the Ethidium homodimer can cross the disordered region of the dead cell membrane to reach the nucleus and embed the DNA double strand to produce red fluorescence. Therefore, Ethidium homodimer is a relatively sensitive nucleic acid stain that can accurately detect nucleic acids in solution or in decomposing cells. Ethidium homodimer binds DNA, Ex/Em=528/617 nm .
AMP-PCP disodium is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP disodium binding favors the formation of the active homodimer of Hsp90 .
SR11237 (BMS-649) is a potent retinoid X receptor (RXR)-selective agonist that is devoid of any RAR activity. SR11237 can cause RXR/RXR homodimers to form and transactivate a reporter gene containing a RXR-response element .
LG100754 (UVI 2112) is a RXR dimers modulater. LG100754 acts as a RXR:RXRhomodimer antagonist, but functions as a agonist towards RXR:PPARα and RXR:PPARγ heterodimers. LG100754 is an insulin sensitizer that functions through RXR .
Acridine homodimer (NSC 219743), acridine dimer, is a fluorescence dye. Acridine homodimer emits a blue-green fluorescence when bound to DNA. Acridine homodimer has extremely high affinity for AT-rich regions of nucleic acids, can be used for chromosome banding .
TWIK-1/TREK-1-IN-1 (compound 2a) is an inhibitor of the TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.36 μM and 14.6 μM, respectively, and has antidepressant-like effects .
AMP-PCP is an ATP analogue and can bind to Hsp90 N-terminal domain with a Kd value of 3.8 μM. AMP-PCP binding favors the formation of the active homodimer of Hsp90 .
TWIK-1/TREK-1-IN-2 (Compound 2g) is a TWIK-1/TREK-1 inhibitor. TWIK-1/TREK-1-IN-2 inhibits TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 10.13 μM and 15.5 μM. TWIK-1/TREK-1-IN-2 is an antidepressant .
AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
Onfekafusp alfa (L19TNF) is a homotrimer that forms from engineered peptides for the L19 antibody in scFv format fused to human TNF. Onfekafusp alfa can be used for malignant glioma research .
TWIK-1/TREK-1-IN-3 (compound 2h) is an inhibitor of TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.74 μM and 16.5 μM, respectively, and has antidepressant-like effects .
BMS-8 inhibits the PD-1/PD-L1 interaction with IC50 of 7.2 μM. BMS-8, binds directly to PD-L1 and induces formation of PD-L1 homodimers, which in turn prevents the interaction with PD-1 .
L2P4 is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
Thiazole orange dimer YOYO 1 is a green fluorescent dye used for DNA staining. It belongs to the monomethine cyanine dye family and is a tetracationic homodimer of oxazole yellow (abbreviated as YO, hence the name YOYO), usually provided as a tetraiodide salt. In aqueous buffer, the free YOYO-1 dye (λmax 458 nm; λmax 564 nm) has a very low fluorescence quantum yield, but after binding to double-stranded DNA through diintercalation, the fluorescence intensity is increased by 3200 times (λmax 489 nm; λmax 509 nm).
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively . LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy .
Nurr1 agonist 9 (Compound 36) is an agonist for Nurr1 with an EC50 of 0.090 µM and a Kd of 0.17 µM. Nurr1 agonist 9 activates the Nurr1 homodimer (NurRE, EC50=0.094 µM) and the Nurr1-RXR heterodimer (DR5, EC50=0.165 µM). Nurr1 agonist 9 induces the expression of Nurr1-regulated tyrosine hydroxylase (TH) in organoid Parkinson's Disease model. Nurr1 agonist 9 is human brain endothelial cell barrier prmeable .
TH023 is an inhibitor for the TLR4 signaling pathway, that targets especially the formation of TLR4 homodimer. TH023 inhibits secreted embryonic alkaline phosphatase in cell HEK-Blue hTLR4 with an IC50 of 0.354 μM, and inhibits the NO expression in RAW264.7 with an IC50 of 1.61μM. TH023 also inhibits the activation of NF-κB, reduces the nuclear translocation of NF-κB p65. TH023 exhibits anti-inflammatory efficacy in LPS (HY-D1056)-induced mouse acute sepsis model, and ameliorates the mouse lung injury .
On May 15, 2024, "Dimerization and antidepressant recognition at noradrenaline transporter" was published online by Nature. The research findings were an effort from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. This study unraveled the important neural system target - the noradrenaline transporter (NET), obtaining the binding modes of human NET homodimers with the natural substrate norepinephrine (NE) and six selective antidepressants. It laid an important theoretical foundation for understanding the physiological regulation mechanisms of NET and other monoamine transporters.
The Norepinephrine Transporter (NET) Compound Library is obtained by computer-aided virtual screening based on the HY-L901 compound library . The specific screening process includes molecular docking screening, key pharmacophore screening, and CNS-MPO screening, which can be used for new drug discovery targeting the noradrenaline transporter.
Ethidium homodimer (EthD-1) is a high-affinity fluorescent nucleic acid dye commonly used to stain mammals, bacteria, yeast, and fungi. Ethidium homodimer binds to DNA or RNA, enhancing fluorescence more than 30 times. The Ethidium homodimer has a strong positive charge, so it cannot cross cell membranes and stain living cells; But the Ethidium homodimer can cross the disordered region of the dead cell membrane to reach the nucleus and embed the DNA double strand to produce red fluorescence. Therefore, Ethidium homodimer is a relatively sensitive nucleic acid stain that can accurately detect nucleic acids in solution or in decomposing cells. Ethidium homodimer binds DNA, Ex/Em=528/617 nm .
Thiazole orange dimer YOYO 1 is a green fluorescent dye used for DNA staining. It belongs to the monomethine cyanine dye family and is a tetracationic homodimer of oxazole yellow (abbreviated as YO, hence the name YOYO), usually provided as a tetraiodide salt. In aqueous buffer, the free YOYO-1 dye (λmax 458 nm; λmax 564 nm) has a very low fluorescence quantum yield, but after binding to double-stranded DNA through diintercalation, the fluorescence intensity is increased by 3200 times (λmax 489 nm; λmax 509 nm).
L2P4 is a peptide-based and EBNA1 targeting fluorescent probe, which inhibits the EBNA1 homodimer formation and selectively inhibits EBV+ tumor growth. L2P4 exhibits cytotoxicity in EBV-positive C666-1 cell with LC50 of 46.4 μM .
Onfekafusp alfa (L19TNF) is a homotrimer that forms from engineered peptides for the L19 antibody in scFv format fused to human TNF. Onfekafusp alfa can be used for malignant glioma research .
SOD1 Antibody is an unconjugated, approximately 17 kDa, rabbit-derived, anti-SOD1 monoclonal antibody. SOD1 Antibody can be used for: WB, IF-Cell, IF-Tissue, IHC-P, FC expriments in human, mouse, rat background without labeling.
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