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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
140 Results for "
α5
" in MedChemExpress (MCE) Product Catalog:
Products (140)
140 Results for "α5" in MCE Product Catalog:
78
Target:
Cilengitide (EMD 121974) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC50 values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors .
78
Target:
Cilengitide TFA (EMD 121974 TFA) is an integrin (integrin) inhibitor with blood-brain barrier permeability, with IC50 values against human targets as follows: 0.61 nM for αvβ3, 8.4 nM for αvβ5, 14.9 nM for α5β1, 5400 nM for αIIbβ3, 2050 nM for αvβ6, 2350 nM for αvβ8. Cilengitide TFA inhibits the binding of integrins to vitronectin, fibronectin, fibrinogen and LAP (TGF-β), and serves as an internal standard for solid-phase integrin binding assays. Cilengitide TFA inhibits tumor cell viability, induces apoptosis, reduces the phosphorylation levels of STAT3, AKT and mTOR, downregulates the expression of PD-L1, inhibits cell viability and angiogenesis, regulates anti-tumor immune responses and slows tumor growth. Cilengitide TFA can be used in research related to glioblastoma, melanoma, advanced solid tumors and refractory brain tumors .
12
12 Cited Publications
Synonyms: ATN-161 TFA salt
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
12
12 Cited Publications
Cat. No.: HY-13535
CAS No.: 262438-43-7
Research Areas:
Cardiovascular Disease Infection Neurological Disease Cancer
ATN-161 is an antagonist of α5β1 integrin and αvβ3 integrin, as well as an inhibitor of fibrosis, an inhibitor of oxidative stress, a tight junction stabilizer, a mitochondrial integrity protector, an angiogenesis inhibitor and an antiviral agent. ATN-161 inhibits NLRP3, MAPK, and ROS. ATN-161 protects mice from SARS-CoV-2 infection . ATN-161 reduces infarct volume, alleviates edema, decreases immune cell infiltration, reduces the area of choroidal neovascularization lesions, lowers tumor microvessel density and viral load. ATN-161 can be used in research related to ischemic stroke, choroidal neovascularization, breast cancer, coronavirus disease 2019 (COVID-19), and liver metastasis of colorectal cancer [5].
11
11 Cited Publications
Cat. No.: HY-P1740
CAS No.: 114681-65-1
Research Areas:
11
11 Cited Publications
Cat. No.: HY-P1740A
Research Areas:
8
8 Cited Publications
Synonyms: Ro 13-7410; Arotinoid acid; AGN191183
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
8
Target:
Research Areas:
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively .
5
Target:
Research Areas:
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a molecular glue that induces the targeted degradation of splicing factor RBM39 by recruiting the E3 ubiquitin ligase CUL4-RBX1-DDB1-DCAF15 (CRL4 DCAF15). E7820 is an angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. E7820 can be used for the study of acute myeloid leukemia (AML) .
4
4 Cited Publications
Target:
Research Areas:
L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
4
3
Target:
Research Areas:
3
Target:
Research Areas:
Padsevonil (UCB0942) is a potent antiepileptic agent that selectively acts on presynaptic and postsynaptic targets. Padsevonil binds to synaptic vesicular protein 2 (SV2) with high affinity. Padsevonil is also a positive allosteric modulator and partial agonist of GABAAR, with high potency against α1 and α5 receptors. Padsevonil has antiepileptic effects in a variety of rodent models .
2
Target:
Research Areas:
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
2
2 Cited Publications
Synonyms: S44819; Egis-13529
Target:
Research Areas:
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy .
2
2 Cited Publications
Target:
Research Areas:
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
1
1 Cited Publications
Synonyms: Lu 02-030 hydrochloride; THIP hydrochloride
Target:
Research Areas:
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
1
1 Cited Publications
Cat. No.: HY-175287
CAS No.: 3115530-47-4
α5β1 integrin agonist-2 (Compound 2) is a selective α5β1 integrin agonist (EC50 = 45.98 nM). α5β1 integrin agonist-2 induces integrin activation. α5β1 integrin agonist-2 is applicable to the research of leukemia .
1
1 Cited Publications
Cat. No.: HY-P77718
Purity: ≥ 95%, as determined by reducing SDS-PAGE or Bis-Tris PAGE.
Synonyms: ITGA5; Integrin Alpha-F; Prev. FNRA; CDNA FLJ50382, Moderately Similar To Integrin Alpha-5; CD49e; Very Late Activation Protein 5, Alpha Subunit; Integrin, Alpha 5 (Fibronectin Receptor, Alpha Polypeptide); Fibronectin Receptor, Alpha Subunit; Fibronectin
Species:
Human
Source:
HEK293
1
1 Cited Publications
Cat. No.: HY-P70845A
Purity: ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: MOG; MOG Alpha-5; Myelin Oligodendrocyte Glycoprotein; MOG AluA; Myelin-Oligodendrocyte Glycoprotein; MOG AluB; BTNL11; MOGIG2; BTN6; NRCLP7; MOG Ig-AluB
Species:
Human
Source:
HEK293
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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
