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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
157 Results for "
Checkpoint inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (157)
157 Results for "Checkpoint inhibitor" in MCE Product Catalog:
5
5 Cited Publications
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SB-218078 is a potent, selective, ATP-competitive and cell-permeable checkpoint kinase 1 (Chk1) inhibitor that inhibits Chk1 phosphorylation of cdc25C with an IC50 of 15 nM. SB-218078 is less potently inhibits Cdc2 (IC50 of 250 nM) and PKC (IC50 of 1000 nM). SB-218078 causes apoptosis by DNA damage and cell cycle arrest .
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5 Cited Publications
Cat. No.: HY-18175
CAS No.: 1404095-34-6
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CCT244747 is a potent, orally bioavailable and highly selective CHK1 inhibitor, with an IC50 of 7.7 nM; CCT244747 also abrogates G2 checkpoint with an IC50 of 29 nM.
3
3 Cited Publications
BOS-172722 is an inhibitor of monopolar spindle 1 (MPS1) checkpoint with an IC50 of 11 nM and 63 nM for MPS1 (1 mM ATP) and P-MPS1, respectively. BOS-172722 also has potential for the study of various forms of breast cancer .
2
2 Cited Publications
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity .
2
2 Cited Publications
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CA-170 is an orally delivered dual inhibitor of VISTA and PD-L1. CA-170 exhibits potent rescue of proliferation and effector functions of T cells inhibited by PD-L1/L2 and VISTA with selectivity over other immune checkpoint proteins as well as a broad panel of receptors and enzymes .
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2 Cited Publications
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SirReal2 is a potent, isotype-selective Sirt2 inhibitor with an IC50 value of 140 nM and has very little effect on the activities of Sirt3-5. SirReal2 leads to tubulin hyperacetylation in HeLa cells and induces destabilization of the checkpoint protein BubR1. SirReal2 combined with VS-5584 (HY-16585) suppresses tumor growth and extends the survival rate of mice in tumor xenograft model. SirReal2 is is promising for research of cancer, inflammation and neurodegeneration .
1
1 Cited Publications
Synonyms: ZIO 301; D 24851
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Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis .
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1
1 Cited Publications
KIF18A-IN-1 is an inhibitor of the mitotic kinesin KIF18A with anti-tumor activity. KIF18A targeted inhibitors may activate mitotic checkpoints and selectively kill chromosomally unstable cancer cells .
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1 Cited Publications
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M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC) .
1
1 Cited Publications
Cat. No.: HY-131446
CAS No.: 2120398-39-0
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Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model .
1
1 Cited Publications
Cat. No.: HY-P99144A
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Cat. No.: HY-P9986
CAS No.: 1918185-84-8
Synonyms: MTIG-7192A; RG-6058
Cat. No.: HY-P99166
CAS No.: 2329669-72-7
Synonyms: XMAB-20717
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Cat. No.: HY-P99950
CAS No.: 2484949-51-9
Synonyms: ALX148
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JBI-589 is a non-covalent PAD4 isoform-selective inhibitor with oral bioavailability. JBI-589 reduces CXCR2 expression and blocks neutrophil chemotaxis. JBI-589 reduces primary tumor and metastases, and enhances the anti-tumor effect of checkpoint inhibitors. JBI-589 can be used in cancer research .
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BMS-1001 is an orally active human PD-L1/PD-1 immune checkpoint inhibitor. BMS-1001 exhibits low-toxicity in cells. The IC50 value of BMS-1001 in a homogeneous time-resolved fluorescence (HTRF) binding assay is 2.25 nM .
Synonyms: CR6086
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Vorbipiprant (CR6086) is an orally active EP4 receptor antagonist with high selectivity for the human EP4 receptor (Ki: 16.6 nM). Vorbipiprant has immunomodulatory, anti-inflammatory, antitumor, and anti-angiogenic activities. Vorbipiprant can inhibit the expression of multiple pro-inflammatory cytokines and the activation of immune cells, and convert "cold" tumors unresponsive to immune checkpoint inhibitors into "hot" tumors. Vorbipiprant is used in the research of diseases such as rheumatoid arthritis and colon cancer .
Cat. No.: HY-P99895
CAS No.: 2417124-95-7
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Cat. No.: HY-18961
CAS No.: 622864-54-4
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PD 407824 is a checkpoint kinase Chk1 and WEE1 inhibitor with IC50s of 47 and 97 nM, respectively. PD 407824 is a chemical BMP sensitizer and increases the sensitivity of cells to sub-threshold amounts of BMP4 .
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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
