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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
102 Results for "
abrogates
" in MedChemExpress (MCE) Product Catalog:
Products (102)
102 Results for "abrogates" in MCE Product Catalog:
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(S,R)-GSK321 is the (S,R)-enantiomer of GSK321 (HY-18948). GSK321 is a potent, selective mutant IDH1 inhibitor with IC50 values of 2.9, 3.8, 4.6 and 46 nM for R132G, R132C, R132H and WT IDH1, respectively, and >100-fold selectivity over IDH2. GSK321 induces decrease in intracellular 2-HG, abrogation of the myeloid differentiation block and induction of granulocytic differentiation at the level of leukemic blasts and more immature stem-like cells. GSK321can be used for research of acute myeloid leukemia (AML) and other cancers .
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Cat. No.: HY-126278
CAS No.: 2375374-15-3
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Z1609609733 (Compound 18) is a non-covalent 3-Phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 1.46 μM. Z1609609733 significantly inhibits serine synthesis and cancer metabolism with complete abrogation of cell proliferation .
Cat. No.: HY-P99723
CAS No.: 2168561-26-8
Synonyms: BCD-135
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Cat. No.: HY-171230
CAS No.: 2803422-60-6
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MTH1 activator-1 is an MTH1 activator that enhances endogenous MTH1 activity and significantly reduces 8-oxo-dG levels in cellular DNA. MTH1 activator-1 can be used to probe the cellular and biological effects of upregulated oxidative damage repair in nucleotide pools and to delay or abrogate tumorigenesis .
Cat. No.: HY-P3709
CAS No.: 852805-92-6
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Cat. No.: HY-100313
CAS No.: 182959-28-0
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Cat. No.: HY-178190
WEE1-IN-13 (Compound 10) is a highly selective WEE1 kinase inhibitor (IC50=0.7 nM). WEE1-IN-13 abrogates the G2/M checkpoint and induces tumor cell apoptosis. WEE1-IN-13 is promising for research of solid tumors (e.g., non-small cell lung cancer, ovarian cancer) .
Cat. No.: HY-145785
CAS No.: 2227429-65-2
ADH-6 is a tripyridylamide compound. ADH-6 abrogates self-assembly of the aggregation-nucleating subdomain of mutant p53 DBD. ADH-6 targets and dissociates mutant p53 aggregates in human cancer cells, which restores p53's transcriptional activity, leading to cell cycle arrest and apoptosis. ADH-6 has the potential for the research of cancer diseases[1].
Cat. No.: HY-110347
CAS No.: 1883548-93-3
Mps1-IN-1 dihydrochloride is a potent and ATP-competitive Mps1 kinase inhibitor with an IC50 of 367 nM. Mps1-IN-1 dihydrochloride inhibit Mps1 mitotic kinase activity and abrogates spindle assembly checkpoint (SAC) function. Mps1-IN-1 dihydrochloride decreases the viability of both cancer and ‘normal’ cells .
Cat. No.: HY-16129A
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Cat. No.: HY-P4978
CAS No.: 1351804-17-5
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Cat. No.: HY-P3709A
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Cat. No.: HY-175448
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GNE-1567 is a potent ERα PROTAC degrader and a XIAP antagonist with a Kd of 0.03 μM. GNE-1567 induces ubiquitination and degradation of ERα by recruiting the E3 ubiquitin ligase XIAP, thereby achieving the dual effects of ERα protein elimination and abrogation of XIAP-mediated apoptosis inhibition simultaneously. GNE-1567 can be used in studies related to ERα-dependent breast cancer .
Cat. No.: HY-161838
ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.
Cat. No.: HY-164445
CAS No.: 2591440-71-8
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STAT3-IN-32 is an orally active, selective STAT3 SH2 domain inhibitor with a Kd of 21.3 nM, showing selectivity over STAT1/5. STAT3-IN-32 binds to the STAT3 SH2 domain, blocks Tyr705 and Ser727 phosphorylation, abrogates nuclear transcription and mitochondrial oxidative phosphorylation functions. STAT3-IN-32 inhibits tumor growth in mouse pancreatic cancer xenograft models. STAT3-IN-32 can be used for the research of pancreatic cancer .
Synonyms: U-99194A; PNU-99194A maleate; JPC-211 maleate
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U-99194 (PNU-99194) maleate is a selective, potent dopamine D3 receptor antagonist (Ki =160 nM). U-99194 maleate inhibits the activation of D3 receptor mediated by endogenously released dopamine or exogenous D3 agonists. U-99194 maleate abrogates the IPSC-suppressive effect of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 maleate significantly suppresses Nicotine (HY-127019)-induced tremor in mice. U-99194 maleate can be used for the study of dopamine D3 receptor-mediated motor disorders, particularly kinetic tremors .
Cat. No.: HY-177785
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iDeg-6 is a molecular glue degrader that selectively targets IDO1, with a DC50 of 6.5 nM, an IC50 of 16 nM, and a Kd of 1.46 μM. iDeg-6 competes to bind the heme-binding site of apoprotein IDO1, promoting CRL2 KLHDC3-mediated polyubiquitination of IDO1 and neddylation-modification-dependent proteasomal degradation. iDeg-6 reduces kynurenine production, abrogates the non-enzymatic pro-tumor migration function of IDO1, and inhibits tumor growth in immunodeficient mice. iDeg-6 can be used in studies of cancer, infection, and neurological diseases (such as melanoma) .
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LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer .
Cat. No.: HY-P991582
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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
