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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
45 Results for "
KRAS^{G12V}
" in MedChemExpress (MCE) Product Catalog:
Products (45)
45 Results for "KRAS^{G12V}" in MCE Product Catalog:
18
18 Publications Verification
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
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Target:
PROTACs FKBP Epigenetic Reader Domain HDAC Histone Methyltransferase c-Myc Polo-like Kinase (PLK) Ras MHC
Research Areas:
FKBP12 PROTAC dTAG-7 (dTAG-7) is a FKBP12 F36V PROTAC degrader. FKBP12 PROTAC dTAG-7 binds FKBP12 F36V and CRBN to form a complex, mediating degradation via the ubiquitin-proteasome system. FKBP12 PROTAC dTAG-7 mediates the degradation of FKBP12 F36V-tagged nuclear and cytoplasmic proteins, including BRD4, HDAC1, EZH2, MYC, PLK1, KRAS G12V, and antigen fusion proteins. FKBP12 PROTAC dTAG-7 enhances MHC class I antigen presentation. FKBP12 PROTAC dTAG-7 is applicable to leukemia-related research .
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1 Cited Publications
Cat. No.: HY-159652
CAS No.: 2920695-77-6
KRAS inhibitor-31 (compound 33) is a KRAS inhibitor, with KD (SPR) values of 0.019 nM, 0.019 nM and 0.096 nM for KRas G12D, KRas G12C and KRas G12V, respectively .
Cat. No.: HY-173632
CAS No.: 3040175-17-2
AMG410 is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 can be used for the study of colorectal, pancreatic, and lung cancers .
Cat. No.: HY-173629
CAS No.: 3082166-76-2
RMC-5127 is a small molecule inhibitor that binds to GTP-targeted KRAS G12V, with oral bioavailability and blood-brain barrier permeability. RMC-5127 inhibits the activities of the RAS and MAPK pathways, suppresses the proliferation of KRAS G12V-mutant cancer cells and induces their apoptosis. RMC-5127 can be used for the research of KRAS G12V-mutant non-small cell lung cancer, pancreatic ductal adenocarcinoma, colorectal cancer and intracranial KRAS G12V tumors .
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-159788
CAS No.: 2938169-99-2
PROTAC K-Ras Degrader-4 (Compound 4) is a PROTAC degrader for KRAS that degrades KRAS G12D in GP5d and degrades KRAS G12V in cell SW620 with DC50s of 1 nM and 13 nM. PROTAC K-Ras Degrader-4 inhibits MAPK signaling pathway .
Cat. No.: HY-176954
CAS No.: 2171015-78-2
Target:
Research Areas:
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-179253
CAS No.: 3079342-05-2
Cat. No.: HY-159474
CAS No.: 3030576-47-4
KRAS inhibitor-24 (compound 115c) is a pyridopyrimidine KRAS inhibitor, with an IC50 of < 100 nM for KRas G12V, KRas WT and KRas G12R .
Cat. No.: HY-P11356
CAS No.: 1932689-39-8
Cat. No.: HY-P11356A
Cat. No.: HY-178042
CAS No.: 2756257-56-2
SS-3091 is a pan-KRas inhibitor active across KRas G12D, KRas G12C, KRas G12V, KRas G12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRas G12 mutations. SS-3091 can be used for the research of KRas-driven cancers .
Cat. No.: HY-147099
Purity: 97.8%
dTAG-47-NEG is an inactive bifunctional negative control PROTAC and also the diastereomer of dTAGV-1 (HY-145514D). dTAG-47-NEG does not reduce the level of BCL11A-FKBP12 F36V, nor does it induce the degradation of BCL11A-FKBP12 F36V, proteins tagged with FKBP12 F36V, wild-type FKBP12, FKBP12 F36V-KRAS G12V or FKBP12 F36V-EWS/FLI. dTAG-47-NEG exerts no antiproliferative effect in cancer cells .
Cat. No.: HY-169311
CAS No.: 3058573-95-5
KRAS inhibitor-37 (compound 2) is a potent KRAS inhibitor with KDs of 0.004 nM, 0.041 nM, 0.019 nM and 0.144 nM for KRAS wild type, KRAS G12D, KRAS G12C and KRAS G12V by SPR binding assay, respectively. KRAS inhibitor-37 inhibits cell proliferation with IC50s of <2 nM-14 nM for H358, SW620, PANC08.13 cells, respectively. KRAS inhibitor-37 has the potential for cancer research .
Cat. No.: HY-179300A
CAS No.: 3074833-87-4
KRAS-IN-48 (Compound 1-01) is a KRAS mutant inhibitor, with Kd values of 2.58 nM and 5.49 μM for KRAS-G12D and KRAS-G12V, respectively. KRAS-IN-48 can be used in the research of cancer .
Cat. No.: HY-164365
CAS No.: 3043670-74-9
PROTAC K-Ras degrader-2 (compound 48) is a KRAS G12V PROTAC degrader with an IC50 of 20-200 nM for KRAS G12V/RAF1. PROTAC K-Ras degrader-2 degrades SW620 KRAS G12V with a DC50 of 1-10 nM. PROTAC K-Ras degrader-2 inhibits cell growth of SW620 3D cell with an IC50 of ≤10 nM. PROTAC K-Ras degrader-2 can be used for the study of colorectal cancer (CRC) .
Cat. No.: HY-173329
CAS No.: 3056974-50-3
KRAS-IN-41 is an inhibitor of KRAS with IC50 values of <0.01 μM for KRAS G12D and KRAS G12V. KRAS-IN-41 inhibits RAS mutant cell lines, GP2D (KRAS-G12D) and SW620 (KRAS-G12V). KRAS-IN-41 can be used in cancer research .
Cat. No.: HY-176250
KRAS-IN-43 (Compound 9) is a pan-KRAS inhibitor with IC50 values of 0.15 μM, 0.14 μM, and 0.47 μM against KRAS G12V, KRAS G12C and wild-type KRAS, respectively. KRAS-IN-43 disrupts the interaction between KRAS and cRAF, and inhibits ERK phosphorylation. KRAS-IN-43 is promising for research of KRAS mutation-related cancers (such as pancreatic cancer, colorectal cancer, and lung cancer) .
Cat. No.: HY-174261
CAS No.: 3082412-00-5
KRAS-IN-5 (Compound Ex 6) is an orally active and selective inhibitor targeting KRAS mutants (including KRAS G12D, KRAS G12V, KRAS WT) with a GNE IC50 value of 1.3 nM against KRAS G12D. KRAS-IN-5 blocks tumor cell proliferation by inhibiting KRAS-mediated signaling pathways (e.g., reducing ERK phosphorylation). KRAS-IN-5 is promising for research of KRAS mutation-related cancers, such as pancreatic cancer, colorectal cancer, lung 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
