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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
156 Results for "
RNA-binding cleft
" in MedChemExpress (MCE) Product Catalog:
Products (156)
156 Results for "RNA-binding cleft" in MCE Product Catalog:
26
26 Publications Verification
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Endocrinology Cancer
IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
9
Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
9
Target:
Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis
Research Areas:
Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
4
4 Cited Publications
Target:
Research Areas:
Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 μM. Ro 08-2750 inhibits NGF binding to p75 NTR selectively over TRKA . Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM .
2
Target:
Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing .
2
2 Cited Publications
Cat. No.: HY-B0268A
CAS No.: 84294-96-2
Synonyms: Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate
Target:
Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing .
2
2 Cited Publications
CMLD-2, an inhibitor of HuR-ARE interaction, competitively binds HuR protein disrupting its interaction with adenine-uridine rich elements (ARE)-containing mRNAs (Ki=350 nM). CMLD-2 induces apoptosis exhibits antitumor activity in different cancer cells as colon, pancreatic, thyroid and lung cancer cell lines. Hu antigen R (HuR) is an RNA binding protein, can regulate target mRNAs stability and translation .
2
2 Cited Publications
Target:
Research Areas:
(R)-SKBG-1 is a covalent inhibitor targeting the RNA binding protein NONO. (R)-SKBG-1 can reduce the expression of androgen receptor (AR) and its splice variants, inhibiting cancer cell proliferation. (R)-SKBG-1 inhibits androgen receptor expression with IC50 of 3.1 μM and 5.5 μM for AR-FL mRNA and AR-V7 mRNA, respectively. (R)-SKBG-1 interferes with the gene regulatory network of cancer cells and inhibits cancer cell growth by stabilizing the interaction between NONO and mRNA. (R)-SKBG-1 can be used in the study of cancers related to NONO dysfunction, such as prostate cancer .
1
1 Cited Publications
Cat. No.: HY-174228
CAS No.: 552829-57-9
Target:
Research Areas:
I3IN-002 is a small-molecule RNA-binding protein IGF2BP3 inhibitor with an IC50 value of approximately 2 μM in SEM cells. I3IN-002 interferes with interaction with m6 A-modified mRNAs, disrupting the stabilization of target genes (such as CDK6, MYC, and BCL2) to inhibit leukemic cell growth, induce cell cycle arrest, and promote apoptosis. I3IN-002 is promising for research of B-cell acute lymphoblastic leukemia .
1
1 Cited Publications
KH-3 is a potent RNA-binding protein Hu antigen R (HuR) inhibitor with an IC50 value of 0.35 μM. KH-3 has anti-proliferative activity. KH-3 suppresses breast cancer cell invasion as well as delays the initiation of lung colonies by disrupting HuR-FOXQ1 mRNA interaction .
1
1 Cited Publications
Target:
Research Areas:
Anticancer agent 73 (compound CIB-3b) is a anticancer agent, potently targeting TAR RNA-binding protein 2 (TRBP) and disrupts its interaction with Dicer. Anticancer agent 73 can rebalance the expression profile of oncogenic or tumor-suppressive miRNAs. Anticancer agent 73 suppresses the proliferation and metastasis of HCC in vitro and in vivo .
1
1 Cited Publications
Cat. No.: HY-P72145
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: CIRBP; Glycine-Rich RNA binding Protein; Cold Inducible RNA binding Protein; A18 HnRNP; Cold-Inducible RNA-binding Protein; Cold Inducible RNA-binding Protein; CIRP; Testicular Tissue Protein Li 39; Glycine-Rich RNA-binding Protein CIRP; A18HNRNP
Species:
Mouse
Source:
E. coli
1
1 Cited Publications
Cat. No.: HY-A0022A
CAS No.: 63302-99-8
Synonyms: Azafen monohydrate; Pipofezin dihydrochloride monohydrate; Pipofezine dihydrochloride monohydrate
Target:
Research Areas:
Azaphen dihydrochloride monohydrate is an orally active tricyclic antidepressant that inhibits the reuptake of serotonin and monoamines, regulates the 5-HT2c receptor, and exerts sedative, antidepressant and anxiolytic effects. Azaphen dihydrochloride monohydrate increases the bioavailability of serotonin in the synaptic cleft, does not block muscarinic receptors or affect monoamine oxidase activity, and binds to the human serotonin transporter via salt bridges, π-stacking, π-cation and hydrophobic interactions. Azaphen dihydrochloride monohydrate can be used in studies related to depression .
Cat. No.: HY-P5960
Synonyms: PTBP1 α3-helix derived peptide P6 TFA
Target:
Research Areas:
Target:
Environmental Pollutants Apoptosis Insecticide Cholinesterase (ChE) Reactive Oxygen Species (ROS)
Research Areas:
Carbaryl is the inhibitor for acetylcholinesterase that inhibits the degradation of acetylcholine in the synaptic cleft, leads to the accumulation of acetylcholine and causes neurotoxicity. Carbaryl can be used as an insecticide .
Cat. No.: HY-175238
CAS No.: 1309288-83-2
Target:
Research Areas:
KI-DX-014 is a DDX21 inhibitor with high RNA-binding inhibitory activity (IC50 of 3.31 μM). KI-DX-014 targets DDX21’s intrinsically disordered C-terminal domain, inhibits DDX21-structured RNA interaction, modulates DDX21’s RNA-dependent ATPase activity, and disrupts DDX21 biomolecular condensate formation. KI-DX-014 attenuates in vitro P-TEFb release from the 7SK snRNP complex, suppresses P-TEFb-dependent RNA polymerase II CTD phosphorylation, and induces developmental defects in zebrafish embryos. KI-DX-014 acts as a chemical probe for dissecting DDX21 functions in normal physiology and disease states. KI-DX-014 can be used for cancers and neurodegenerative disorders research .
Cat. No.: HY-163759
CAS No.: 3040301-46-7
Target:
Research Areas:
HuR degrader 2 is a molecular glue degrader targeting HuR (ELAVL1). HuR degrader 2 degrades the RNA-binding protein HuR. HuR degrader 2 can be used for the research of pancreatic ductal adenocarcinoma .
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Research Areas:
Gossypolone is an RNA-binding protein Musashi-1 inhibitor with a Ki of 12 nM. Gossypolone disrupts the Musashi-numb RNA interaction and directly binds to the RBD1 of MSI1 protein. Gossypolone can be used for the research of cancer .
Target:
Research Areas:
zr17-2 is a cold inducible RNA-binding protein (CIRBP) agonist. zr17-2 has anti-inflammatory and anti-oxidant and can be used for the study of myocardial infarction. zr17-2 is a hypothermia mimetic molecule that reduces oxidative stress-induced retinal cell death .
Cat. No.: HY-124844
CAS No.: 1448460-87-4
Synonyms: AZA-9
Azaphilone-9 (AZA-9) is an inhibitor of HuR-ARE RNA interaction (IC50=1.2 μM) by binding RNA-binding protein Hu antigen R (HuR). The HuR-RNA interactions stabilize many oncogenic mRNAs in tumors. Thus Azaphilone-9 potentially inhibit cancer cell growth and progression .
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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
