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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
143 Results for "
Switch 2 closure
" in MedChemExpress (MCE) Product Catalog:
Products (143)
143 Results for "Switch 2 closure" in MCE Product Catalog:
62
62 Publications Verification
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations [2].
60
Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis.
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13 Cited Publications
Art. -Nr.: HY-U00451
CAS. Nr.: 1847485-97-5
11
11
11 Cited Publications
Synonyms: SP-2577
Target:
Forschungsgebiete:
Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma [2].
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11 Cited Publications
Synonyms: SP-2577 mesylate
Target:
Forschungsgebiete:
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma [2].
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9 Cited Publications
Synonyms: DCC-2618
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) [2]. DCC-2618 exerts antineoplastic effect and induces apoptosis .
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9
9 Cited Publications
Art. -Nr.: HY-114164H
CAS. Nr.: 9002-04-4
Synonyms: EC 3.4.21.5 (Lyophilized); Human Alpha Thrombin (Lyophilized)
Forschungsgebiete:
Human α-Thrombin (EC 3.4.21.5; Human Alpha Thrombin) (Lyophilized) is a terminal serine protease in the coagulation cascade, as well as a potent physiological platelet agonist and fibrin-generating enzyme in vivo. Human α-Thrombin catalyzes the conversion of fibrinogen to fibrin for blood clot formation, and activates platelet aggregation by cleaving the protease-activated receptors PAR1 (major) (Kd = 1 nM) and PAR4 (minor) on the platelet surface to expose tethered ligands. Human α-Thrombin also amplifies coagulation via positive feedback by activating coagulation factors V, VIII, XI (FV/FVIII/FXI), and switches to activate protein C to exert anticoagulant effects after binding to thrombomodulin [2] .
This product is in a freeze-dried form.
This product is in a freeze-dried form.
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6 Cited Publications
Synonyms: GDC-6036
Divarasib (GDC-6036) is an orally active, selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds Cys12 in GDP-bound KRAS G12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib induces tumor shrinkage and robust tumor growth inhibition in KRAS G12C-positive models and cancer cells. Divarasib can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRAS G12C-mutated solid tumors [2] .
6
Divarasib (GDC-6036) adipate is an orally active, selective KRASG12C inhibitor with an IC50 of <0.01 μM. Divarasib adipate covalently binds Cys12 in GDP-bound KRASG12C, occupies the switch II pocket, blocks GTP binding and SOS-mediated reactivation, and inhibits oncogenic KRAS signaling. Divarasib adipate induces tumor shrinkage and robust tumor growth inhibition in KRASG12C-positive models and cancer cells. Divarasib adipate can be used for the research of non-small cell lung cancer, colorectal adenocarcinoma, pancreatic ductal adenocarcinoma, and other KRASG12C-mutated solid tumors [2] .
5
5 Cited Publications
Target:
Forschungsgebiete:
ZINC40099027 is a selective FAK activator. ZINC40099027 promotes FAK phosphorylation, without activating its paralogs Pyk2 and Src. ZINC40099027 promotes the wound closure of human intestinal epithelial monolayers and the healing of mouse ulcers by activating FAK. ZINC40099027 can be used for diseases related to gastrointestinal mucosal injury research .
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3 Cited Publications
Target:
Forschungsgebiete:
Rheb inhibitor NR1 is a Rheb inhibitor with an IC50 of 2.1 µM in the Rheb-IVK assay. Rheb inhibitor NR1 can directly bind Rheb in the switch II domain and selectively inhibit the activation of mechanistic target of rapamycin complex 1 (mTORC1). Rheb inhibitor NR1 inhibits the phosphorylation of mTORC1 driven T389pS6K1 and increases the phosphorylation of S473pAKT in a dose-dependent manner. Rheb inhibitor NR1 does not influence mTORC2 activity .
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
(Rheb-IVK: Rheb-dependent mTORC1 kinase activity)
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Category:
Infection Colophony Ketones, Aldehydes, Acids Metabolic Disease Plants Pinaceae Extract Disease Research Fields Inflammation/Immunology
Target:
2
1
Target:
Forschungsgebiete:
1
1 Cited Publications
Art. -Nr.: HY-18604
CAS. Nr.: 1629265-17-3
K-Ras G12C-IN-1 is an irreversible covalent KRAS G12C inhibitor. K-Ras G12C-IN-1 contains an electrophilic group that forms an irreversible covalent bond with Cys12 of mutant K-Ras. After covalent binding to Cys12, it locks Switch II in an inactive state and interferes with downstream Ras signaling. K-Ras G12C-IN-1 can be used in research related to pancreatic cancer, colon cancer, MYH-associated polyposis, colorectal cancer, and lung cancer .
1
Art. -Nr.: HY-N11420
CAS. Nr.: 62251-96-1
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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
