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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
270 Results for "
Checkpoint
" in MedChemExpress (MCE) Product Catalog:
Products (270)
270 Results for "Checkpoint" in MCE Product Catalog:
Cat. No.: HY-162259
CAS No.: 3032646-96-8
Research Areas:
QC-182 is a p300/CBP PROTAC degrader with a DC50 of 93 nM against p300. QC-182 induces ubiquitination and proteasomal degradation of p300 and CBP in a CRBN-dependent manner. QC-182 induces Apoptosis. QC-182 exhibits anticancer activity against liver cancer cells. QC-182 can be used for the research of hepatocellular carcinoma .
Cat. No.: HY-184918
CAS No.: 3097045-01-4
Target:
Research Areas:
NAMPT/PD-1/PD-L1-IN-1 is a potent the PD-1/PD-L1 interaction and NAMPT dual inhibitor with IC50s of 7.5 nM and 18.8 nM, respectively. NAMPT/PD-1/PD-L1-IN-1 enhances T cell-mediated tumor cell killing, promotes T cell proliferation and CD8 + T cell proportion and depletes intracellular NAD + biosynthesis. NAMPT/PD-1/PD-L1-IN-1 suppresses tumor progression in a mouse LLC xenograft model by disrupting tumor metabolism and activating the tumor immune microenvironment. NAMPT/PD-1/PD-L1-IN-1 can be used in research on tumor immunotherapy for non-small cell lung cancer .
Cat. No.: HY-P990569
CAS No.: 1783801-93-3
Synonyms: MK-6018
Target:
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Cat. No.: HY-P991942
Synonyms: BAY3375968; TPP-23411
Target:
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Cat. No.: HY-119225
CAS No.: 67427-51-4
Target:
Research Areas:
CBP-93872 is a G2 checkpoint inhibitor and a chemosensitizer. CBP-93872 specifically inhibits DNA double-strand break (DSB)-dependent, Nbs1-mediated ATR activation, without directly inhibiting ATR kinase activity or affecting ATR activation induced by other types of DNA damage; meanwhile, it suppresses the pathway between ATM and ATR activation, thereby reducing the autophosphorylation of ATR and the subsequent phosphorylation of Chk1. CBP-93872 does not inhibit DNA end resection at DSB sites. CBP-93872 induces cell death and enhances the cytotoxic effects of platinum-containing compounds and pyrimidine antimetabolites on cancer cells. CBP-93872 can be used in related research on p53-mutant cancers, colorectal cancer, and pancreatic cancer .
Research Areas:
Apcin-A is a small molecule inhibitor that selectively targets the cell division cycle protein Cdc20 and is a derivative of Apcin (HY-110287). Apcin-A competitively binds to the D-box binding pocket of Cdc20 and inhibits substrate ubiquitination mediated by the anaphase promoting complex APC/C-Cdc20. Apcin-A also blocks the binding of Cdc20 to substrates (such as securin and cyclin B1), inhibiting anaphase initiation and cell cycle exit. Apcin-A can promote or prolong mitotic slippage in coordination with p31 comet under conditions of high spindle assembly checkpoint (SAC) activity. Apcin-A can be used to develop anti-mitotic drugs and overcome tumor chemotherapy resistance. Apcin-A can be used to synthesize PROTAC CP5V (HY-130257)[1][2][3].
Cat. No.: HY-169232
Target:
Research Areas:
Cat. No.: HY-181838
CAS No.: 3064485-73-7
CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer .
Cat. No.: HY-P705896
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: WEE1; WEE1 G2 Checkpoint Kinase; Wee1-Like Protein Kinase; WEE1A; Wee1A Kinase; WEE1hu; Non-Specific Protein-Tyrosine Kinase; Wee1+ (S. Pombe) Homolog; WEE1 Homolog (S. Pombe); Protein Kinase; WEE1+ Homolog; WEE1 Homolog
Species:
Human
Source:
sf9 insect cells
Cat. No.: HY-P701865
Purity: ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: TRIP13; PCH2; Pachytene Checkpoint protein 2 homolog; Human papillomavirus type 16 E1 protein-binding protein; 16E1-BP; HPV16 E1 protein-binding protein; Thyroid hormone receptor interactor 13; Thyroid receptor-interacting protein 13; TR-interacting prote
Species:
Human
Source:
E. coli
Cat. No.: HY-P702928
Purity: ≥ 85%, as determined by reducing SDS-PAGE.
Synonyms: BUB1; Budding Uninhibited By Benzimidazoles 1 (Yeast Homolog); Prev. BUB1L; BUB1 Budding Uninhibited By Benzimidazoles 1 Homolog; HBUB1; Budding Uninhibited By Benzimidazoles 1 Homolog; BUB1A; Putative Serine/Threonine-Protein Kinase; Mitotic Checkpoint S
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-P706113
Purity: ≥ 85%, as determined by reducing SDS-PAGE.
Synonyms: WEE1; WEE1 G2 Checkpoint Kinase; Wee1-Like Protein Kinase; WEE1A; Wee1A Kinase; WEE1hu; Non-Specific Protein-Tyrosine Kinase; Wee1+ (S. Pombe) Homolog; WEE1 Homolog (S. Pombe); Protein Kinase; WEE1+ Homolog; WEE1 Homolog
Species:
Human
Source:
Sf9 insect cells
Cat. No.: HY-116470
CAS No.: 1202055-39-7
Mps1/TTK-IN-1 (Compound cpd-5), a derivative of NMS-P715 (HY-12382), is a Mps1 kinase inhibitor with an IC50 of 9.2 nM and a Kd of 1.6 nM. Mps1/TTK-IN-1 specifically targets the ATP-binding pocket of the Mps1 kinase. Mps1/TTK-IN-1 maintains inhibitory activity against Mps1 drug-resistant mutants (C604Y, C604W) with IC50 values of 170 and 19 nM and Kd values of 471 and 349 nM. Mps1/TTK-IN-1 can block the phosphorylation of kinetochore protein KNL1 mediated by Mps1, interfere with the spindle assembly checkpoint function, prevent the correct separation of chromosomes, and thereby inhibit the mitosis and proliferation of tumor cells .
Cat. No.: HY-168739
CAS No.: 2413582-45-1
Target:
Topoisomerase Reactive Oxygen Species (ROS) Apoptosis Survivin Bcl-2 Family IAP DNA/RNA Synthesis
Research Areas:
Topoisomerase I inhibitor 17 (Compound 7h) is a Topoisomerase I (Top1) inhibitor. Topoisomerase I inhibitor 17 reduces DDX5 and reverses the locking of Top1 activity by DDX5. Topoisomerase I inhibitor 17 induces Top1-mediated DNA damage and promotes reactive oxygen species (ROS) production. Topoisomerase I inhibitor 17 induces Apoptosis (reduces antiapoptotic proteins XIAP, Bcl-2, Survivin and up-regulates pro-apoptotic proteins Bax, γH2AX). Topoisomerase I inhibitor 17 also blocks the progression of the G2/M checkpoint and induces cell cycle arrest. Topoisomerase I inhibitor 17 significantly inhibits colony formation and cell migration in colorectal cancer cells. Topoisomerase I inhibitor 17 effectively reduces tumors in human PDX tumor mice .
Cat. No.: HY-184299
Target:
Research Areas:
PD-1/PD-L1-IN-65 is a PD-1/PD-L1 checkpoint inhibitor, with an EC50 of 6.06 μM for blocking the PD-1/PD-L1 interaction and a Kd of 1.43 μM for PD-L1. PD-1/PD-L1-IN-65 upregulates pro-inflammatory cytokines IFN-γ, IL-1α, IL-1β and the cytolytic protein perforin, and reverses T cell exhaustion. PD-1/PD-L1-IN-65 enhances T cell-mediated cancer cell lysis. PD-1/PD-L1-IN-65 can be used in the research of breast cancer .
Cat. No.: HY-19926A
CAS No.: 1778671-05-8
Synonyms: RG-7602 hydrochloride
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GDC-0425 hydrochloride (RG-7602 hydrochloride) is an orally active, highly selective ChK1 inhibitor. GDC-0425 hydrochloride abrogates cell cycle arrest and inhibits genomic repair. GDC-0425 hydrochloride potently suppresses Gemcitabine (HY-17026)-induced pCDK1/2 expression. GDC-0425 hydrochloride can be used in research related to osteosarcoma, ovarian cancer, basal (triple-negative) breast cancer, and colorectal cancer .
Cat. No.: HY-P992314
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Cat. No.: HY-15532A
CAS No.: 891495-88-8
Synonyms: (Rac)-MK-8776
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(Rac)-SCH900776 ((Rac)-MK-8776) is the racemate of SCH900776 (HY-15532). SCH900776 (MK-8776) is a potent and selective Chk1 inhibitor with an IC50 value of 3 nM .
Cat. No.: HY-P991181
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Cat. No.: HY-123597
CAS No.: 15427-93-7
Synonyms: DDUG; NCI C04808
Target:
Research Areas:
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
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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
