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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
20 Results for "
kinome kinases
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "kinome kinases" in MCE Product Catalog:
36
36 Publications Verification
Synonyms: BMS-986165
3
3 Cited Publications
Cat. No.: HY-15985
CAS No.: 1439934-41-4
Target:
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CTX-0294885 is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
3
3 Cited Publications
Cat. No.: HY-15985A
CAS No.: 2319590-02-6
Target:
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CTX-0294885 hydrochloride is a broad spectrum kinase inhibitor that can capture 235 kinases from MDA-MB-231 cells, and can capture all members of the AKT family. CTX-0294885 hydrochloride is a powerful reagent for analysis of kinome signaling networks that can be used for the research of diseases like inflammation, diabetes, and cancer .
BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. BI-4020 inhibits not only the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR del19 T790M and primary mutant EGFR del19 (IC50=1 nM). BI-4020 also shows activity against EGFR wt (IC50=190 nM). BI-4020 shows high kinome selectivity and good DMPK properties .
Cat. No.: HY-162426
CAS No.: 3069333-33-8
UNC-CA2-103 is a TLK2 inhibitor with a human IC50 of 18 nM, and it exhibits high selectivity over TLK1 and the vast majority of other kinases. UNC-CA2-103 can be used in research related to breast cancer, glioblastoma and gastric cancer .
Cat. No.: HY-172429
CAS No.: 2489185-38-6
Synonyms: ORIC-114
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Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1 .
Cat. No.: HY-172429A
Synonyms: ORIC-114 hemihydrate
Target:
Research Areas:
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
Cat. No.: HY-176205
CAS No.: 3024588-48-2
Synonyms: AB801
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Ligritinib (AB801) is an orally active AXL receptor tyrosine kinase inhibitor, with a IC50 of 1.8 nM, Ki of 0.024 nM, and Kd of 0.093 nM against human targets. It exhibits broad selectivity against the human kinome, including high selectivity for MERTK and TYRO3. Ligritinib blocks the AXL signaling pathway independent of dimerization inducers, and acts as both a tumor growth inhibitor and an AXL inducer. Ligritinib can be used in research related to clear cell renal cell carcinoma, advanced solid tumors, and non-small cell lung cancer .
Cat. No.: HY-15268
CAS No.: 1092787-12-6
PP487 is a selective dual inhibitor of Tyrosine kinase/PI3-K, with IC50 values of 0.017 μM, 0.072 μM, 0.004 μM, 0.01 μM, 0.55 μM, 0.22 μM, and < 0.01 μM against DNA-PK, mTOR, Hck, Src, EGFR, EphB4, and PDGFR, respectively. PP487 can be used in cancer research .
Cat. No.: HY-173191
CAS No.: 2760404-50-8
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SK-124 is an orally active salt-inducible kinase (SIK) inhibitor with an IC50 of 230 nM against SIK1, 4.1 nM against SIK2, and 21 nM against SIK3, exhibiting excellent kinome selectivity . SK-124 blocks SIK-mediated CRTC2 phosphorylation, promotes CRTC2 nuclear translocation, and regulates vitamin D metabolism by upregulating renal Cyp27b1 and downregulating Cyp24a1 . SK-124 upregulates the expression of bone-related genes, increases serum Ca 2+, 1,25-vitamin D and intact FGF23 levels, and suppresses endogenous PTH levels . SK-124 can be used in studies related to osteoporosis, male osteoporosis, and chronic kidney disease-mineral and bone disorder .
Cat. No.: HY-146697
CAS No.: 2416844-79-4
IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies .
Cat. No.: HY-117287A
CAS No.: 1609392-28-0
Synonyms: BMS-986165 (hydrochloride)
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Deucravacitinib (BMS-986165) hydrochloride is an orally active allosteric inhibitor of tyrosine kinase 2 (TYK2), with an IC50 of 0.2 nM and a Ki of 0.02 nM against the JH2 domain of TYK2, and it exhibits selectivity over other JAK subtypes and most of the kinome. Deucravacitinib hydrochloride blocks IL-23, IL-12, p-STAT1/3 and Type I IFN signaling, and inhibits Th17/Th1-mediated psoriasis inflammation . Deucravacitinib hydrochloride can be used in research related to moderate-to-severe plaque psoriasis, inflammatory bowel disease and systemic lupus erythematosus .
Cat. No.: HY-182043
CAS No.: 2999638-62-7
BLU-654 is an orally active antineoplastic agent and KIT inhibitor. BLU-654 is a highly selective inhibitor targeting wild-type KIT, PDGFRβ, and KIT V654A over most other kinases in the kinome. BLU-654 exerts sustained antineoplastic activity in KIT V654A cell-derived xenograft mouse models. BLU-654 can be used in research related to Imatinib (HY-15463)-resistant gastrointestinal stromal tumors .
Cat. No.: HY-10339A
CAS No.: 841258-76-2
(E)-KW-2449 is a subtype-selective type II kinase inhibitor .
Cat. No.: HY-183584
Target:
Research Areas:
ARN25699 is a kinase inhibitor with an IC50 of 5.5 nM against GSK-3β, 2.2 nM against FYN-α, and 242.3 nM against DYRK1A, and it exhibits oral bioavailability. ARN25699 reduces hyperphosphorylation of tau protein and promotes microtubule bundle formation. ARN25699 has a broader kinome inhibitory profile and targets kinases associated with the pathogenic mechanisms linked to Alzheimer's disease. ARN25699 can be used in the research of Alzheimer's disease and related tauopathies .
Cat. No.: HY-187351
CAS No.: 3132799-96-0
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BMX-IN-4 is a covalent BMX kinase inhibitor with an IC50 of 1.78 nM and a Ki of 0.158 μM. BMX-IN-4 forms a covalent bond with BMX kinase. BMX-IN-4 is applicable to the research of hepatocellular carcinoma .
Cat. No.: HY-103566A
CAS No.: 338738-57-1
Research Areas:
LY456236 free base is a selective, non-competitive and orally active antagonist of glutamate receptor 1 (mGlu1), which can inhibit phosphatidylinositol hydrolysis with an IC50 of 0.145 μM. LY456236 free base can also inhibit EGFR, with an IC50 of 0.918 μM. LY456236 free base blocks cell proliferation by inhibiting the MAPK pathway, reversing the anti-apoptotic effect of DHPG (HY-12598A). LY456236 free base can be used in epilepsy research .
Cat. No.: HY-184004
Research Areas:
NUCC-0231068 is a MNK1 and MNK2 inhibitor with IC50 values of 8 nM and 7 nM, respectively. NUCC-0231068 inhibits the phosphorylation of eukaryotic translation initiation factor 4E (eIF4E) at Ser209, with an IC50 of 23 nM in its purified form and 17 nM in its D2B form. NUCC-0231068 can be used in studies related to glioblastoma .
Cat. No.: HY-181699
ULK1-IN-5 (Compound D1) is a selective ULK1 inhibitor with an IC50 of 14.91 nM. ULK1-IN-5 functionally inhibits the kinase activity of ULK1. ULK1-IN-5 reduces the phosphorylation level of ATG13. ULK1-IN-5 exerts antiproliferative effects on cervical cancer cells. ULK1-IN-5 is applicable to relevant research on cervical cancer .
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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
