Scientific Reviews
Product Guides
Blogs
Topics
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
615 Results for "
Targeted Protein Degradation
" in MedChemExpress (MCE) Product Catalog:
Products (615)
615 Results for "Targeted Protein Degradation" in MCE Product Catalog:
15
15 Publications Verification
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects .
12
12 Cited Publications
Synonyms: GX15-070 Mesylate
Target:
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity .
12
Target:
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2 . Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity .
6
6 Cited Publications
dTAGV-1 TFA is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 TFA induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 TFA is applicable to functional validation studies of cancer and undegradable oncoproteins .
6
6 Cited Publications
dTAGV-1 hydrochloride is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 hydrochloride induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 hydrochloride is applicable to functional validation studies of cancer and undegradable oncoproteins .
6
6 Cited Publications
Cat. No.: HY-145514D
CAS No.: 2451573-86-5
dTAGV-1 is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 is applicable to functional validation studies of cancer and undegradable oncoproteins .
4
4 Cited Publications
Cat. No.: HY-N0242
CAS No.: 28808-62-0
Category:
Dictamnus dasycarpus Turcz. Terpenoids Sesquiterpenes Rutaceae Plants Disease Research Fields Inflammation/Immunology
Target:
4
Category:
Antifungal Marine natural products Anti-parasitic Disease Research Infection Microorganisms Macrolide Antibiotics Antibiotics Phenols Polyphenols Disease Research Fields Marine microorganism
Target:
3
3 Cited Publications
Synonyms: NX-5948; BTK-IN-24
Research Areas:
Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
2
2 Cited Publications
Synonyms: IPI 1040 sodium; TBC11251 sodium
Target:
Research Areas:
Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC50 of 1.4 nM and a Ki of 0.43 nM. Sitaxsentan sodium exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
2
2 Cited Publications
Target:
Research Areas:
PROTAC HK2 Degrader-1 is a PROTAC consisting of Lonidamine (HY-B0486) as a target protein Hexokinase 2 (HK2) inhibitor and Thalidomide (HY-14658) as a CRBN ligand-linked PROTAC. PROTAC HK2 Degrader-1 selectively inhibits the proliferation of breast cancer cells by forming a ternary complex through the ubiquitin-proteasome system to degrade Hexokinase 2 (HK2) protein leading to mitochondrial damage and cell death. PROTAC HK2 Degrader-1 effectively inhibits breast tumor growth and reduces the colonic side effects of cisplatin for breast cancer research .
2
2 Cited Publications
Cat. No.: HY-19726
CAS No.: 803647-40-7
NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway . NSC59984 acts by targeting GOF-mutant p53 and stimulates p73 to restore the p53 pathway signaling .
2
2 Cited Publications
Target:
Research Areas:
EGA is an inhibitor that selectively targets the endosomal trafficking pathways. EGA targets the proteins involved in the endosomal trafficking pathways through which multiple toxins and viruses enter cells. EGA exerts its activity by inhibiting the trafficking from early endosomes to late endosomes, blocking the entry of multiple acid-dependent bacterial toxins and viruses into mammalian cells and delaying the lysosomal targeting and degradation of EGFR .
2
2 Cited Publications
Synonyms: ARV-766; JSB462
Target:
Research Areas:
Luxdegalutamide (ARV-766) is an orally active protein hydrolysis targeted chimeric (PROTAC) targeting androgen receptor (AR), which can degrade AR resistance related mutants, including T878/H875/L702 mutants. Luxdegalutamide has anti-tumor activity and can be used in the study of castration resistant prostate cancer .
2
2 Cited Publications
Research Areas:
HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).
2
2 Cited Publications
Target:
Research Areas:
BETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia .
1
1 Cited Publications
Target:
Research Areas:
PROTAC RIPK degraders -2 is a non-peptide PROTAC based on von Hippel-Lindau and targets serine-threonine kinase RIPK2, which is highly selective to the degradation of RIPK2. PROTAC RIPK degrader-2 acts as an activator to increase cell death and activate ion channels in cancer cells. PROTAC RIPK degrader-2 also can inhibit protein interactions, such as receptors and ligands, involved in a variety of diseases, such as cancer and diabetes .
1
1 Cited Publications
Cat. No.: HY-175324
CAS No.: 3098773-64-6
Target:
Research Areas:
MG-HuR2 is a molecular glue degrader targeting the oncogenic RNA-binding protein HuR (IC50=0.5 μM). MG-HuR2 is promising for research of HuR-overexpressing malignancies (e.g., breast cancer) .
1
1
1 Cited Publications
Cat. No.: HY-153713
Purity: 98.05%
MYC-RIBOTAC is a nucleic acid-targeting degrader (ribonuclease-targeting chimera, RIBOTAC) that targets the MYC internal ribosome entry site (IRES). MYC-RIBOTAC contains a MYC mRNA binding component and a small molecule that recruits and locally activates RNAse L1. MYC-RIBOTAC reduces MYC mRNA and protein expression levels, induces cell apoptosis, and can be used for antitumor research . MYC-RIBOTAC consists of pre-miR-155 binder Anticancer agent 167 (HY-156839), RNA binder NCI-B16 (HY-156215), and Linker Amino-PEG4-alcohol (HY-W008005).
-
-
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
