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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
588 Results for "
pol -in-5
" in MedChemExpress (MCE) Product Catalog:
Products (588)
588 Results for "pol -in-5" in MCE Product Catalog:
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2 Cited Publications
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Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis .
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CAY10499 (MAGL-IN-5) is a non-selective lipase inhibitor with IC50 values of 144 nM and 14 nM for monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), respectively. Additionally, CAY10499 exhibits anti-inflammatory and antiviral activities .
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2 Cited Publications
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
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2 Cited Publications
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Dot1L-IN-5 is a potent disruptor of telomeric silencing 1-like protein (DOT1L) inhibitor with an IC50 of 0.17 nM .
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LY-3381916 (IDO1-IN-5) is a potent, selective and brain penetrated inhibitor of IDO1 activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1 .
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2 Cited Publications
Synonyms: (R)-Enitociclib; (-)-BAY-1251152; (-)-VIP152
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(-)-Enitociclib ((R)-Enitociclib) is an enantiomer of Enitociclib (HY-103019E) with an optical rotation of (-). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC + lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies .
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Tambiciclib (GFH009, JSH-009) is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib can be used for AML research .
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1 Cited Publications
Cat. No.: HY-N2566
CAS No.: 53155-25-2
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1 Cited Publications
Cat. No.: HY-162859
CAS No.: 2565637-94-5
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AB25583 is a Polθ helicase (Polθ-hel) small molecule inhibitor, with an IC50 value of 6 nM. AB25583 selectively kills BRCA1/2 deficient cells and works in synergy with Olaparib (HY-10162) in cancer cells carrying pathogenic BRCA1/2 mutations. AB25583 can be used for tumor research .
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1 Cited Publications
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TGFβ-IN-5 is a type I transforming growth factor-β receptor (TGF-β R1) kinase inhibitor with an IC50 value of 0.0485 μM. TGFβ-IN-5 reverses the effect of TGF-β-mediated cell activation on the expression of fibrosis-related genes. TGFβ-IN-5 can be used in the research of fibroproliferative diseases .
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1 Cited Publications
Cat. No.: HY-X0009A
CAS No.: 2559759-04-3
Synonyms: GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleate
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Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A/B, and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC, and inducing apoptosis. Tambiciclib dimaleate can be used for AML research .
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1 Cited Publications
Cat. No.: HY-147803
Purity: 98.07%
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TrxR-IN-5 (compound 4f) is a potent TrxR (thioredoxin reductase) inhibitor, with an IC50 of 0.16 μM. TrxR-IN-5 increases the levels of ROS, thus leading to potent antiproliferative effects. TrxR-IN-5 exhibits prominent anticacer and anti-metastasis effects .
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1 Cited Publications
Cat. No.: HY-164714
CAS No.: 308830-70-8
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HSL-IN-5 (Example 21) is a hormone sensitive lipase (HSL) inhibitor (IC50: 0.25 μM). HSL-IN-5 can be used for diabetes research .
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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 .
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1 Cited Publications
PARP1-IN-5 dihydrochloride is a low toxicity, orally active, potent and selective PARP-1 inhibitor (IC50 =14.7 nM). PARP1-IN-5 dihydrochloride can be used for the research of cancer .
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1
1 Cited Publications
FGFR3-IN-5 is a potent and selective FGFR3 inhibitor with IC50 values of 3, 44, and 289 nM for FGFR3, FGFR2, and FGFR1, respectively. FGFR3-IN-5 can be used in research of cancer .
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1 Cited Publications
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GPX4-IN-5 is a covalent inhibitor of GPX4 (IC50: 0.12 μM). GPX4-IN-5 can induce ferroptosis and has anti-tumor effects. GPX4-IN-5 can be used in the study of triple-negative breast cancer (TNBC) .
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1 Cited Publications
Cat. No.: HY-163299
CAS No.: 3027172-23-9
pan-KRAS-IN-5 is a pan-KRAS translation inhibitor by targeting 5′-UTR RNA G-quadruplexes (rG4s). pan-KRAS-IN-5 strongly binds to and stabilizes KRAS rG4s, inhibits KRAS translation, and blocks the MAPK and PI3K-AKT pathways. pan-KRAS-IN-5 induces cell cycle arrest, prompts apoptosis in KRAS-driven cancer cells. pan-KRAS-IN-5 inhibits tumor growth and KRAS expression in KRAS-mutant xenograft. KRAS-IN-5 can be used for KRAS-driven cancer research .
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1 Cited Publications
Cat. No.: HY-172158
CAS No.: 140481-05-6
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ALKBH5-IN-5 is a highly selective ALKBH5 (IC50 = 0.62 μM, Kd = 804 nM). ALKBH5-IN-5 disrupts ALKBH5 binding to m 6A-RNA and 6mA-DNA substrates. ALKBH5-IN-5 promotes differentiation, induces apoptosis, cause G2-M phase arrest and exerts strong antiproliferative effects in cancer cells. ALKBH5-IN-5 reduces TACC3 and MYC protein levels and increases cleaved caspase-3 levels. ALKBH5-IN-5 exerts antitumor activity in tumor xenograft mice models. ALKBH5-IN-5 can be used for the research of acute myeloid leukemia .
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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
