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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
94 Results for "
switchable
" in MedChemExpress (MCE) Product Catalog:
Products (94)
94 Results for "switchable" in MCE Product Catalog:
Cat. No.: HY-D3269
CAS No.: 2088127-60-8
Cat. No.: HY-114894
CAS No.: 2230185-95-0
2C07 is a mutant Ras (K-Ras M72C, H-Ras M72C) inhibitor. 2C07 blocks the activation of PI3K through allosteric Ras modification. 2C07 binds to the modified switch II pocket (S-IIG) of Ras in both GDP- and GTP-bound states, stabilizes the GDP-bound state, disrupts the polar interactions of the canonical GTP-bound state, and inhibits SOS binding and nucleotide exchange. 2C07 can be used in cancer-related research .
Cat. No.: HY-D3130
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Mem-pH is a ratiometric fluorescent probe used for measuring vesicular pH. Mem-pH inserts into the plasma membrane bilayer and localizes to the vesicular lumen, switching between its basic and acidic forms via protonation during vesicular acidification to enable ratiometric pH readout. In aqueous media, Mem-pH forms non-emissive aggregates through aggregation-induced quenching, and then depolymerizes and recovers its fluorescent activity upon binding to the plasma membrane. The excitation/emission wavelengths of the basic form of Mem-pH are 405/450-550 nm, while those of the acidic form are 488/500-700 nm .
Cat. No.: HY-D3164
CAS No.: 1380316-56-2
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TPE-Cy is a fluorescent probe with both aggregation-induced emission (AIE) property and pH-dependent luminescent behavior. TPE-Cy exhibits significant luminescent differences under different acidic and alkaline conditions: it shows moderate to strong red emission with linear variation with pH in acidic environments and within the pH range of 5-7, weak or even no emission within the pH range of 7-10, and switches to blue emission under alkaline conditions. TPE-Cy possesses excellent cell permeability and biocompatibility, enabling accurate ratiometric pH sensing and imaging monitoring in living cells via confocal microscopy, ratiometric analysis and flow cytometry .
Cat. No.: HY-186001
CAS No.: 2922732-38-3
Synonyms: RM-044
RMC-9945 (RM-044) is a selective, covalent, and orally active RAS (ON) G12D inhibitor. RMC-9945 enhances the transcriptional activity of β-Catenin/TCF. RMC-9945 induces cell state transition, forcing metastatic colorectal cancer cells to switch from the Emp1 + state to the Lgr5 + stem cell-like state. RMC-9945 achieves durable disease control in preclinical models of colorectal cancer with early liver metastasis, but shows reduced activity in late-stage metastasis models. RMC-9945 can be used in research related to metastatic colorectal cancer and pancreatic ductal adenocarcinoma .
Cat. No.: HY-177192
CAS No.: 64023-32-1
Synonyms: DMPS
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1,2-Dimyristoyl-sn-glycero-3-phosphoserine (DMPS) is an anionic, negatively charged phosphatidylserine phospholipid. 1,2-Dimyristoyl-sn-glycero-3-phosphoserine acts as an internal standard for liquid chromatography/mass spectrometry analyses .
Cat. No.: HY-165459
CAS No.: 401907-57-1
Synonyms: MK-056
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KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (Ki=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus .
Cat. No.: HY-186223
CAS No.: 897375-76-7
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Enzyme modulator-1 (example 205) is a potent enzyme modulator that modulates p38, bcr-ab1, and VEGFR. Enzyme modulator-1 can be used for the research of cancer, rheumatoid arthritis, retinopathies including diabetic retinal neuropathy and macular degeneration .
Cat. No.: HY-181420A
CAS No.: 3029443-36-2
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BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-189129
RAS GTPase-IN-3 is a RAS GTPase inhibitor that targets multiple KRAS-Q61 mutant variants. RAS GTPase-IN-3 binds to the switch II pocket of GTP-bound KRAS-Q61R, positions its side-chain imidazole group near the GTP γ-phosphate, and accelerates GTP hydrolysis of KRAS-Q61. RAS GTPase-IN-3 inhibits Sos-catalyzed nucleotide exchange on GTP-bound KRAS. RAS GTPase-IN-3 only activates GTP hydrolysis of HRAS-Q61R/Q95H and NRAS-Q61R/L95H mutant proteins. RAS GTPase-IN-3 can be applied in research related to cancers driven by KRAS-Q61 mutations .
Cat. No.: HY-P11892
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c10c-G1V3 is a BRAG2 binder with a Kd value of 7.37 μM. c10c-G1V3 binds to BRAG2, thereby disrupting its interaction with GluA2 and blocking GluA2 endocytosis and AMPAR subunit switching. c10c-G1V3 reduces glutamate-induced intracellular reactive oxygen species (ROS) accumulation and cell apoptosis (apoptosis). c10c-G1V3 decreases infarct volume in the transient middle cerebral artery occlusion model. c10c-G1V3 can be used in studies related to ischemic stroke .
Cat. No.: HY-134813R
CAS No.: 2621928-55-8
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MRTX1133 (Standard) is the analytical standard of MRTX1133 (HY-134813). This product is intended for research and analytical applications. 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 .
Cat. No.: HY-181420
CAS No.: 3029184-80-0
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(S,R,S)-BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). (S,R,S)-BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. (S,R,S)-BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. (S,R,S)-BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. (S,R,S)-BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-L260
82 compounds
KRAS (Kirsten Rat Sarcoma Viral Oncogene Homolog) is one of the most important oncogenic driver genes in oncology, with high mutation frequencies in pancreatic cancer, non‑small cell lung cancer, and colorectal cancer. For a long time, KRAS was considered "undruggable" due to the lack of suitable small‑molecule binding pockets on its protein surface. In recent years, with the discovery of the switch‑II pocket and the successful approval of KRAS G12C inhibitors, KRAS‑targeted research has achieved groundbreaking progress, which has also spurred a wave of development targeting non‑G12C mutants such as G12D and G12V, as well as upstream and downstream regulatory factors including SOS1 and SHP2.
MCE KRAS Targeted Compound Library contains 82 small‑molecule compounds targeting the KRAS, serving as high‑quality research tools for mechanistic studies of KRAS‑mutant tumors, combination therapy development, resistance mechanism exploration, and high‑throughput drug screening, thereby providing robust support for KRAS‑targeted drug discovery.
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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
