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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
10796 Results for "
G0/G1-phase,orally active
" in MedChemExpress (MCE) Product Catalog:
Products (10796)
10796 Results for "G0/G1-phase,orally active" in MCE Product Catalog:
627
Target:
Research Areas:
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis [1] .
605
605 Cited Publications
Research Areas:
Y-27632 dihydrochloride is an orally active and ATP-competitive ROCK (Rho-kinase) inhibitor (ROCK-I Ki=220 nM; ROCK-II Ki=300 nM). Y-27632 dihydrochloride shows antiepileptic effects [1] .
387
387 Cited Publications
Synonyms: AZD2281; KU0059436; MK-7339
Research Areas:
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator. Olaparib cannot cross the intact blood-brain barrier (BBB) [1] .
308
308 Cited Publications
Synonyms: GSK1120212; JTP-74057
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis, cross the blood-brain barrier (BBB), used in research related to subarachnoid hemorrhage (SAH) [1] .
308
308 Cited Publications
Synonyms: GSK-1120212 (DMSO solvate); JTP-74057 (DMSO solvate)
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib (DMSO solvate) activates autophagy and induces apoptosis [1] . This product is in solid form, a DMSO solvate, and a stable crystalline form.
223
Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity [1] .
197
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor [1]. Doxycycline shows antibacterial activity and anti-cancer cell proliferation activity [1] .
197
197 Cited Publications
Cat. No.: HY-N0565A
CAS No.: 10592-13-9
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Doxycycline hydrochloride, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor [1]. Doxycycline hydrochloride shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline hydrochloride can be used to construct gene expression regulation models [1] .
197
197 Cited Publications
Cat. No.: HY-N0565B
CAS No.: 24390-14-5
Synonyms: Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
Target:
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Doxycycline hyclate, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor. Doxycycline hyclate shows antibacterial activity and anti-cancer cell proliferation activity. Doxycycline hyclate can be used to construct gene expression regulation models [1] .
197
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer [1] .
197
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM), with blood-brain barrier permeability. Rosiglitazone is an TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer [1] .
194
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer [1] .
191
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Research Areas:
Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester proagent of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy.
162
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Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM [1].
131
131 Cited Publications
Cat. No.: HY-50946
CAS No.: 220127-57-1
Synonyms: STI571 Mesylate; CGP-57148B Mesylate
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Imatinib Mesylate (STI571 Mesylate) is an orally active tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
126
126 Cited Publications
Synonyms: RAD001; SDZ-RAD
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective, orally active, blood-brain barrier-permeable mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities [1] .
117
117 Cited Publications
STM2457 is a first-in-class, highly potent, selective and orally active METTL3 inhibitor with an IC50 of 16.9 nM. STM2457 can be used for the research of acute myeloid leukaemia (AML) [1] .
113
Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity [1].
112
112 Cited Publications
Synonyms: PF-07321332
Target:
Research Areas:
Nirmatrelvir (PF-07321332) is a potent and orally active SARS-CoV 3C-like protease (3CL PRO) inhibitor. Nirmatrelvir (PF-07321332) targets to the SARS-CoV-2 virus and can be used for COVID-19 research [1].
112
112 Cited Publications
Synonyms: L593754 hydrochloride; MH 12-43 hydrochloride; Ethylisopropylamiloride hydrochloride
Research Areas:
EIPA (L593754) hydrochloride is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA hydrochloride also enhances autophagy by inhibiting Na +/H +-exchanger 3 (NHE3). EIPA hydrochloride inhibits macropinocytosis as well. EIPA hydrochloride can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma [1] .
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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
