Search Result
Results for "
subnanomolar
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13674
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NSC 153858
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Microtubule/Tubulin
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Cancer
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Maytansine is a highly potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at subnanomolar concentrations .
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- HY-107725
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Neuropeptide Y Receptor
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Metabolic Disease
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BIBO3304, a chemical probe, is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively) .
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- HY-P99294
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AMG 479; Human Anti-IGF1R Recombinant Antibody
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IGF-1R
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Cancer
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Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
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- HY-P991734
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TREM receptor
Syk
Calcium Channel
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Neurological Disease
Inflammation/Immunology
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VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
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- HY-14221A
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Lu 28-179 hydrochloride
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Sigma Receptor
Ferroptosis
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Cancer
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Siramesine (Lu 28-179) hydrochloride is a potent sigma-2 receptor agonist. Siramesine hydrochloride has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine hydrochloride triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
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- HY-14221
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Lu 28-179
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Sigma Receptor
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Cancer
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Siramesine (Lu 28-179) is a potent sigma-2 receptor agonist. Siramesine has a subnanomolar affinity for sigma-2 receptors (IC50=0.12 nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17 nM). Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
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- HY-P99172
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CD47
Interleukin Related
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Cancer
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CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors .
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- HY-107365
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PI3K
mTOR
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Cancer
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PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .
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- HY-149648
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RSV
DNA/RNA Synthesis
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Infection
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JNJ-8003 is a potent and orally active non-nucleoside RSV polymerase inhibitor with an IC50 of 0.29 nM. JNJ-8003 targets the L protein polymerase complex of RSV (IC50 = 0.67 nM), and blocks the transcription and replication of the viral genome by inhibiting the activity of RNA-dependent RNA polymerase (RdRp). JNJ-8003 displays subnanomolar activity in vitro as well as prominent efficacy in mice and a neonatal lamb models. JNJ-8003 can be used for the study of respiratory syncytial virus (RSV) .
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- HY-160696
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CD73
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Cancer
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ORIC-533 is an orally active, highly selective, AMP-competitive CD73 inhibitor that potently blocks adenosine production with sub-nanomolar affinity (Ka=0.03 nM). In multiple myeloma, ORIC-533 restores and enhances the cytotoxicity of the immune system against tumor cells through multiple immunological mechanisms, including reversing the immunosuppressive microenvironment, inducing immunogenic cell death, and activating dendritic cells, T cells and NK cells, with no direct toxicity to normal cells. The combination of ORIC-533 with Daratumumab (HY-P9915) synergistically enhances anti-tumor efficacy, significantly increases intratumoral CD8 + T cell infiltration and inhibits tumor growth in vivo .
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- HY-19936A
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Bacterial
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Infection
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ACHN-975 TFA is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 TFA is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL) .
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- HY-P2274
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Parasite
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Infection
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Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
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- HY-19936
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Bacterial
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Infection
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ACHN-975 is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL) .
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- HY-P2249
-
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Arrestin
Apelin Receptor (APJ)
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Cardiovascular Disease
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ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .
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- HY-P1818
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- HY-120096
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Neuropeptide Y Receptor
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Neurological Disease
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BIBO3304 free base is a nonpeptide neuropeptide Y Y1 receptor antagonist. BIBO3304 free base displays subnanomolar affinity for both the human and the rat Y1 receptor, with IC50 values of 0.38 nM and 0.72 nM, respectively. BIBO3304 free base significantly inhibits food intake induced by application of NPY or by fasting .
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- HY-118423
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IQP-0410
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HIV
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Inflammation/Immunology
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SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase . SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism .
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- HY-U00302
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mAChR
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Inflammation/Immunology
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CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity .
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- HY-P2434
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Somatostatin Receptor
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Neurological Disease
Metabolic Disease
Cancer
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AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research .
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- HY-121352
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Drug Derivative
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Cancer
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Kibdelone C is a hexacyclic tetrahydroxanthone natural product and anticancer agent with sub-nanomolar GI50 activity against human SR leukemia and SN12C renal carcinoma cell lines. Kibdelone C disrupts the actin cytoskeleton in human cancer cells, leading to cell contraction and actin stress fiber formation, without direct actin binding, actin polymerization effects, topoisomerase I/II inhibition, or DNA binding. Kibdelone C can be used for the research of leukemia, and renal cell carcinoma .
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- HY-19210
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Endothelin Receptor
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Cardiovascular Disease
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SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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- HY-153519
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Epigenetic Reader Domain
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Cancer
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WWL0245 is a potent and seletive BRD4 PROTAC. WWL0245 selectively degrades BRD4 with sub-nanomolar DC50 (<1 nM) than BRD2/3 and PLK1 ( DC50>1 μM). WWL0245 shows excellent selective cytotoxicity in the BETi sensitive cancer cell lines, including AR-positive prostate cancer cell lines. WWL0245 is a promising drug candidate for AR-positive prostate cancer research and a valuable tool compound to study the biological function of BRD4 .
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- HY-16622A
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LPL Receptor
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Others
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GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
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- HY-124392
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Phosphodiesterase (PDE)
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Cancer
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AMG580 is a selective PDE10A antagonist with subnanomolar affinity for rat, primate, and human PDE10A. AMG580 can be used for the research of noninvasive radiotracer .
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- HY-135845
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CH0793011
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Topoisomerase
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Cancer
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TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38 . TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro .
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- HY-170420
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JNK
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Others
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JNK-1-IN-5 (Compound 14) is a potent JNK1 inhibitor with sub-nanomolar efficacy. JNK-1-IN-5 suppresses TGF-β-induced epithelial-mesenchymal transition. JNK-1-IN-5 is promising for research of anti-pulmonary fibrosis agent targeting JNK1 .
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- HY-170432
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PARP
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Cancer
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PARP1-IN-34 (compound 30) is a selective PARP1 inhibitor with an IC50 of 0.32 nM. PARP1-IN-34 is a subnanomolar PARP1 inhibitor with >1000-fold selectivity against PARP2 with an IC50 of 326 nM. PARP1-IN-34 shows antitumor efficacy[1].
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- HY-144872
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Drug Derivative
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Cancer
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RJ-34, an aristolactam analogue, exhibits potent antitumor activities against a broad array of cancer cell lines with GI50 values in the subnanomolar range (GI50 <0.1 nM for A431, MES-SA, MES-SA/DX5, HCT-15, and HCT-15/CLO2 cells) .
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- HY-P2274R
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Reference Standards
Parasite
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Infection
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Argifin (Standard) is the analytical standard of Argifin. This product is intended for research and analytical applications. Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
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- HY-170227
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Phosphodiesterase (PDE)
TGF-β Receptor
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Inflammation/Immunology
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Autotaxin-IN-7 (45), a pyridine-2-carboxylic derivative, demonstrates subnanomolar ATX inhibition (IC50 = 0.086 nM), with a favorable heart safety profile (hERG > 30 μM) and minimal fibroblast toxicity. Autotaxin-IN-7 (45) suppresses the TGF-β/Smad signaling pathway, downregulating α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) is used in the research for pulmonary fibrosis .
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- HY-14221B
-
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LU-28-179 fumarate
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Sigma Receptor
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Cancer
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Siramesine (Lu 28-179) fumarate is a potent sigma-2 receptor agonist. Siramesine fumarate has a subnanomolar affinity for sigma-2 receptors (IC50=0.12?nM) and exhibits a 140-fold selectivity for sigma-2 receptors over sigma-1 receptors (IC50=17?nM). Siramesine fumarate triggers cell death through destabilisation of mitochondria, but not lysosomes. Anti-cancer activity .
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- HY-175770
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Isocitrate Dehydrogenase (IDH)
PDK-1
Apoptosis
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Cancer
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mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma .
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- HY-167690
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Endogenous Metabolite
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Infection
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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- HY-185334
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Sodium Channel
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Neurological Disease
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GNE-3565 is an arylsulfonamide class NaV1.7 inhibitor with subnanomolar channel blockage and mixed subtype selectivity.GNE-3565 can be used for the research of pain .
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- HY-112334
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EGFR
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Cancer
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EGFR-IN-198 is a selective EGFR inhibitor with subnanomolar irreversible inhibitory activity against EGFR. EGFR-IN-198 covalently binds to the kinase domain of EGFR and inhibits its autophosphorylation .
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- HY-107725R
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Reference Standards
Neuropeptide Y Receptor
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Metabolic Disease
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BIBO3304 (Standard) is the analytical standard of BIBO3304 (HY-107725). This product is intended for research and analytical applications. BIBO3304, a chemical probe, is a potent, orally active, and selective neuropeptide Y (NPY) Y1 receptor antagonist, with subnanomolar affinity for both the human and the rat Y1 receptor (IC50=0.38 and 0.72 nM, respectively) .
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- HY-107365R
-
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Reference Standards
PI3K
mTOR
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Cancer
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PQR530 (Standard) is the analytical standard of PQR530 (HY-107365). This product is intended for research and analytical applications. PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity .
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- HY-182354
-
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VEGFR
FGFR
FLT3
PDGFR
RET
Akt
ERK
c-Kit
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Cancer
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VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2274
-
|
|
Parasite
|
Infection
|
|
Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively .
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- HY-P2249
-
|
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Arrestin
Apelin Receptor (APJ)
|
Cardiovascular Disease
|
|
ELA-21 (human) is an apelin receptor agonist with a pKi of 8.52. ELA-21 (human) completely inhibits Forskolin-induced cAMP production and stimulates β-arrestin recruitment with subnanomolar potencies. ELA-21 (human) is an agonist in G-protein-dependent and -independent pathways .
|
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- HY-P1818
-
-
- HY-P2434
-
|
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Somatostatin Receptor
|
Neurological Disease
Metabolic Disease
Cancer
|
|
AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research .
|
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- HY-P2274R
-
|
|
Reference Standards
Parasite
|
Infection
|
|
Argifin (Standard) is the analytical standard of Argifin. This product is intended for research and analytical applications. Argifin is a sub-nanomolar chitinase inhibitor produced by soil microorganisms, with IC50s of 0.025 μM, 6.4 μM , 1.1 μM and 4.5 μM for SmChiA (Serratia marcescens chitinaese A), SmChiB, Aspergillus fumigatus chitinase B1 and human chitotriosidase, respectively[1].
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- HY-P5510
-
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HCV NS3 protease substrate
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Peptides
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Others
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Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-ψ-(COO)Ala-Ser-Lys(DABCYL)-NH2 (HCV NS3 protease substrate) is a biological active peptide. (This peptide is a HCV protease substrate incorporating an ester bond between residues P1 and P1. Due to ready transesterification of the scissile bond to the acyl-enzyme intermediate, this substrate shows very high kcat/Km values, enabling detection of activity with subnanomolar nonstructural protein 3 (NS3 protease) concentrations. It is widely used for the continuous assay of NS3 protease activity. Substrate cleavage is proportional to the enzyme concentration with a detection limit for NS3 between 1 nM and 250 pM.
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
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- HY-P99294
-
|
AMG 479; Human Anti-IGF1R Recombinant Antibody
|
IGF-1R
|
Cancer
|
|
Ganitumab (AMG 479) is a recombinant human monoclonal antibody to the human type 1 insulin-like growth factor receptor (IGF1R). Ganitumab recognizes murine IGF1R with sub-nanomolar affinity (KD=0.22 nM) and inhibits the interaction of murine IGF1R with IGF1 and IGF2. Ganitumab can be used in research of cancer .
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(5)
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- HY-P991734
-
|
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TREM receptor
Syk
Calcium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
VHB937 is a potent and selective TREM2 agonist, a human monoclonal antibody, with sub-nanomolar affinity. VHB937 enhances TREM2 surface expression and downstream signaling, such as Syk phosphorylation and calcium mobilization. VHB937 exhibits robust neuroprotective effects in vivo, significantly reducing pathology and pro-inflammatory markers across a broad range of animal models of neuroinflammation and neurodegeneration. VHB937 can be used for neurodegenerative diseases research .
|
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(5)
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- HY-P99172
-
|
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CD47
Interleukin Related
|
Cancer
|
|
CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a high affinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
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Classification |
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- HY-167690
-
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Alkynes
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MK-6186 is a novel non-nucleoside reverse transcriptase inhibitor with sub-nanomolar activity against wild-type viruses and the two most common NNRTI-resistant RT mutants (K103N and Y181C). MK-6186 exhibits excellent antiviral activity against K103N and Y181C mutant viruses. When MK-6186 targets 12 common NNRTI-associated mutant viruses, only two relatively rare mutants (Y188L and V106I/Y188L) show high resistance, with FC values exceeding 100, while the FC values of the remaining viruses are all below 10. In addition, when MK-6186 faces 96 clinical virus isolates carrying NNRTI-resistant mutations, most (70%) viruses show more than 10-fold resistance to efavirenz (EFV), while only 29% of mutant viruses show more than 10-fold resistance to MK-6186 .
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