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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
992 Results for "
degradation activity
" in MedChemExpress (MCE) Product Catalog:
Products (992)
992 Results for "degradation activity" in MCE Product Catalog:
192
192 Publications Verification
Cat. No.: HY-W008923
CAS No.: 17086-28-1
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Doxycycline monohydrate is an orally active highly lipophilic, tissue-permeable MMP inhibitor with broad-spectrum antibacterial activity. Doxycycline monohydrate is also a semi-synthetic antibiotic with chelating properties, which blocks bacterial protein synthesis and inhibits extracellular matrix degradation through interactions with zinc and calcium atoms. Doxycycline monohydrate also inhibits mitochondrial biogenesis, translation, and the expression of respiratory chain proteins. Doxycycline monohydrate induces apoptosis, inhibits autophagy and EMT, downregulates stem cell markers, and activates the PI3K-AKT pathway, thereby effectively inhibiting the viability and proliferation of cancer cells such as breast cancer cells. Doxycycline monohydrate also promotes the survival and self-renewal of embryonic stem cells and neural stem cells, and reduces the frequency of medium changes in culture. Doxycycline monohydrate has been applied in studies related to breast cancer, prostate cancer, bladder cancer, and other cancers .
159
159 Cited Publications
Target:
Research Areas:
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
52
52 Cited Publications
Cat. No.: HY-17439
CAS No.: 55721-31-8
Synonyms: Salinomycin sodium; Sodium salinomycin
Salinomycin sodium salt (Salinomycin sodium), an antibiotic potassium ionophore, is a potent inhibitor of Wnt/β-catenin signaling. Salinomycin sodium salt acts on the Wnt/Fzd/LRP complex, blocks Wnt-induced LRP6 phosphorylation, and causes degradation of the LRP6 protein. Salinomycin sodium salt shows selective activity against human cancer stem cells .
41
41 Cited Publications
Cat. No.: HY-108882C
CAS No.: 9003-98-9
Target:
Research Areas:
DNase I is an enzyme that degrades DNA. DNase I is mainly produced by digestive system organs, such as the pancreas and parotid gland. Three types of DNase I are known in mammals: pancreatic type, parotid type, and pancreatico-parotid type. DNase I plays a key role in the cleavage of extracellular DNA, and is critical for limiting inflammatory responses and maintaining homeostasis. DNase I is responsible for digesting extracellular nucleoproteins, which may be essential for preventing autoimmune reactions. Decreased DNase I activity may be associated with the occurrence and development of systemic lupus erythematosus (SLE). DNase I (filtered) is filtered through a 0.22 μM membrane and is not tested for pyrogenicity .
41
41 Cited Publications
Cat. No.: HY-108882B
CAS No.: 9003-98-9
Target:
Research Areas:
DNase I is an enzyme that degrades DNA. DNase I is mainly produced by digestive system organs, such as the pancreas and parotid gland. Three types of DNase I are known in mammals: pancreatic type, parotid type, and pancreatico-parotid type. DNase I plays a key role in the cleavage of extracellular DNA, and is critical for limiting inflammatory responses and maintaining homeostasis. DNase I is responsible for digesting extracellular nucleoproteins, which may be essential for preventing autoimmune responses. Decreased DNase I activity may be associated with the onset and progression of systemic lupus erythematosus (SLE). DNase I (RNase & Protease free) is a molecular biology-grade DNase I purified by chromatography to remove RNase and protease .
25
25 Cited Publications
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 .
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23 Cited Publications
Target:
Research Areas:
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP .
20
20 Cited Publications
Target:
Research Areas:
CC-885 is a cereblon (CRBN) modulator with potent anti-tumour activity. CC-885 is also a known degrader of GSPT1, inhibiting protein translation.
15
Target:
Research Areas:
Indisulam (E 7070) is a carbonic anhydrase inhibitor with anticancer activity. Indisulam (E 7070) is a sulfonamide agent that targets the G1 phase of the cell cycle. Indisulam (E 7070) causes a blockade in the G1/S transition through inhibition of the activation of both CDK2 and cyclin E. Indisulam (E 7070) targets splicing by inducing RBM39 degradation via recruitment to DCAF15 .
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 .
11
11 Cited Publications
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Research Areas:
ACBI1 is a potent and cooperative SMARCA2, SMARCA4 and PBRM1 degrader with DC50s of 6, 11 and 32 nM, respectively. ACBI1 is a PROTAC degrader. ACBI1 shows anti-proliferative activity. ACBI1 induces apoptosis .
11
11 Cited Publications
Research Areas:
dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP based on Cereblon ligand. dCBP-1 is exceptionally potent at killing multiple myeloma cells and ablates oncogenic enhancer activity driving MYC expression .
11
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Alvelestat (AZD9668) is an orally active, selective inhibitor of neutrophil elastase. Alvelestat reduces elastase activity, myeloperoxidase release, neutrophil recruitment and activation, and calcium phosphate precipitation; promotes smooth muscle cell colonization and collagen deposition; and inhibits the formation of neutrophil extracellular traps (NETs) as well as NET-derived neutrophil elastase activity. Alvelestat restores endothelial dysfunction, regulates antioxidant factors, improves the expression of endothelial tight junctions, reduces vascular leakage, and accelerates wound healing. Alvelestat prevents pulmonary hemorrhage, matrix protein degradation, airspace enlargement, and small airway wall remodeling; and alleviates cigarette-induced inflammatory responses. Alvelestat inhibits the growth of abdominal aortic aneurysms exacerbated by Porphyromonas gingivalis. Alvelestat can be used in research related to chronic obstructive pulmonary disease, abdominal aortic aneurysm, radiation-induced skin injury, and bronchiectasis .
9
9 Cited Publications
SD-36 is a potent and efficacious STAT3 PROTAC degrader (Kd=~50 nM), and demonstrates high selectivity over other STAT members. SD-36 also effectively degrades mutated STAT3 proteins in cells and suppresses the transcriptional activity of STAT3 (IC50=10 nM). SD-36 exerts robust anti-tumor activity, and achieves complete and long-lasting tumor regression in mouse tumor models. SD-36 is composed of the STAT3 inhibitor SI-109, a linker, and an analog of Cereblon ligand Lenalidomide for E3 ubiquitin ligase . SD-36 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
9
9 Cited Publications
Cat. No.: HY-114164F
CAS No.: 9002-04-4
Research Areas:
Canine Thrombin is a Canine serine protease that plays a central role in blood coagulation. Canine Thrombin stimulates macrophages to polarize into a unique phenotype characterized by anti-inflammatory and pro-repair properties. Canine Thrombin activates PAR1, induces the production of MCP-1, MMP3 and VEGF in intervertebral discs, and causes degradation of the cartilage matrix and destruction of intervertebral disc structure. Canine Thrombin activity increases significantly in paraoxon-induced status epilepticus .
8
8 Cited Publications
SKI-II is an oral active and synthetic inhibitor of sphingosine kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteasomal degradation .
7
7 Cited Publications
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research .
6
6 Cited Publications
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity . ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively . ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation .
6
6 Cited Publications
Synonyms: Ribonuclease A; EC 4.6.1.18; RNase A
Target:
Research Areas:
RNase A (Bovine pancreatic RNase) is a widely used Endonuclease in DNA purification by specifically hydrolyzing cytosine or uracil residues of RNA. RNase A degrades the RNA in the RNA/DNA duplex. RNase A catalyses the breakdown of 3',5'-phosphodiester linkages of single stranded RNA. RNase A family members in organisms are tightly involved in various physiological and pathological processes including cell growth and development, proliferation, differentiation and migration. Dysregulation of RNase A activity or expression level is closely related to pancreatic, ovarian, bladder and thyroid cancer. RNase A has tumor cell-killing ability .
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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
