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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
59 Results for "
KRAS-mutant
" in MedChemExpress (MCE) Product Catalog:
Products (59)
59 Results for "KRAS-mutant" in MCE Product Catalog:
19
19 Publications Verification
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DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis .
17
17 Cited Publications
Synonyms: RMC-6236; RAS-IN-2
Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC50 values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors .
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2 Cited Publications
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ML281 is a highly selective inhibitor of serine/threonine kinase 33 (STK33) with an IC50 value of 14 nM. ML281 shows 700-fold selectivity over PKA and 550-fold over AurB. ML281 exerts core mechanism by inhibiting STK33: in small cell lung cancer, ML281 downregulates RPS6/BAD signaling phosphorylation, induces apoptosis, and suppresses proliferation, invasion . ML281 reduces STK33-mediated 4-hydroxyphenylpyruvate dioxygenase (HPD) phosphorylation in tyrosinemia . ML281 is suitable for research on STK33 function, KRAS mutation-related cancers (pancreatic cancer, colon cancer, lung adenocarcinoma, etc.), small cell lung cancer, and tyrosinemia-related damage
1
1 Cited Publications
KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with high affinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
1
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 .
1
1 Cited Publications
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(1S,2S,3R)-DT-061 is an enantiomer of DT-061 (HY-112929). DT-061 is an orally active activator of protein phosphatase 2A (PP2A). (1S,2S,3R)-DT-061 can be used as a negative control in the research of KRAS-mutant and MYC-driven lung cancer tumorigenesis .
ACBI3 (compound 7), a chemical probe, is a PROTAC targeting KRAS. ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models .
BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
Cat. No.: HY-162960
CAS No.: 2937327-83-6
pan-KRAS-IN-18 is a panKRAS inhibitor that inhibits KRAS WT and KRAS G12V with IC50s of 29 and 9 nM, respectively. pan-KRAS-IN-18 exhibits antiproliferative activity in KRAS-mutant cell lines. pan-KRAS-IN-18 can be used for lung cancer research .
Cat. No.: HY-173405
CAS No.: 3055319-82-6
VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer .
Cat. No.: HY-176954
CAS No.: 2171015-78-2
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RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a Kd = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRAS G13D and KRAS G12V cells. RSC-1255 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers .
Cat. No.: HY-176792
CAS No.: 3097985-19-5
ACBI-4 is a selective GTP-loaded active state of KRAS (KRAS(on)) PROTAC degrader, with Kd values of 141 nM against KRAS G12R. ACBI-4 forms a stable ternary complex with VHL, triggering ubiquitination and KRAS degradation via the ubiquitin-proteasome system. ACBI-4 induces antiproliferative effects in KRAS mutant-driven cancer cells. ACBI-4 can be used for the research of KRAS mutant-driven cancer .
Cat. No.: HY-179089
CAS No.: 1884219-70-8
SBP-1750 is an orally active ULK inhibitor and an ATG13 degrader. SBP-1750 strongly inhibits ULK1/2 activity, with IC50 values of 8 and 50 nM, respectively. SBP-1750 induces ATG13 degradation, with an EC50 value of 114 nM. SBP-1750 can inhibit autophagy in cancer cells and induce cell death. SBP-1750 can be used in cancer research, such as for pancreatic cancer .
Cat. No.: HY-159190
CAS No.: 2409140-12-9
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HRX-0233 is an orally potent MAP2K4 inhibitor. HRX-0233 inhibits the MAP2K4-JNK-JUN signaling pathway, blocks the feedback activation of receptor tyrosine kinases, and sustains the inhibitory effect on KRAS signaling. HRX-0233 exerts synergistic inhibition on the mTORC1 and MAPK pathways. When combined with Ipatasertib (HY-15186) or Sotorasib (HY-114277), it produces synergistic antiproliferative, pro-apoptotic (apoptosis) and antitumor effects, and shows good tolerability in mouse models. HRX-0233 can be used in CRISPR knockout screens to identify vulnerability-related genes. HRX-0233 is applicable to research related to prostate cancer, non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-124761
CAS No.: 683808-78-8
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Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors .
Cat. No.: HY-W998345
SMART1 is a highly specific and CRBN-dependent PROTAC that can effectively degrade Smurf1. SMART1 can block the PDK1-Akt signaling pathway in KRAS mutant colorectal cancer. SMART1 can inhibit tumor growth in KRAS mutant colorectal cancer (CRC) xenograft models .
GNE-9815 (compound 7) is a highly selective, pan-RAF inhibitor with good oral bioavailability. GNE-9815 exhibits Ki values of 0.062 and 0.19 nM for CRAF and BRAF, respectively. GNE-9815 combines with MEK inhibitor Cobimetinib (HY-13064) shows synergistic modulation of MAPK pathway. GNE-9815 can be used in studies of KRAS mutant cancers .
Cat. No.: HY-157458
CAS No.: 3054112-59-0
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PDEδ autophagic degrader 1 (compound 12c), an autophagosome-tethering compound (ATTEC). is a potent PDEδ autophagic degrader. PDEδ autophagic degrader 1 reduces the PDEδ protein level through lysosome-mediated autophagy without affecting the PDEδ mRNA expression. PDEδ autophagic degrader 1 suppresses the growth in KRAS mutant pancreatic cancer cells .
Cat. No.: HY-P10436
CAS No.: 2411851-64-2
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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
