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Home > Inhibitors & Agonists > Ras-Raf-MAPK-ERK > Ras

Ras

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Cat. No. Product Name Field of Application Chemical Structure
DC74360 BC-DXI-32982 Featured
BC-DXI-32982 is a potent inhibitor of the interaction between DX2 and KRAS4B with a half-maximal inhibitory concentration (IC50) of 0.18 μM, showing little effect on the PRKACA-PRKAR2A interaction.
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DC70371 DW0254 Featured
DW0254 (DW-0254,DW 0254) is a small molecules capable of inhibiting RAS-related C3 botulinum toxin substrate (RAC) small GTPase activation in ALL cell lines, directly binds to the hydrophobic pocket of PDE6D (Kd=436 nM, ITC), a RAS chaperone protein.DW0254 demonstrated dose-dependent RAC inhibition, arrest of proliferation and induced apoptosis in human leukemic cell lines (RS4;11 IC50=1.5-1.8 uM), also showed promising anti-leukemic activity in RAS-mutated cells (CCRF-CEM NRAS G12D, IC50=3.3-4.2 uM).DW0254 disrupted the interaction between PDE6D and RAS, disturbing RAS subcellular localization.DW0254 demonstrated anti-leukemic activity, decreased tumor progression in a murine xenograft model.
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DC70535 KAL-21404358 Featured
KAL-21404358 (KAL21404358) is a small-molecule, allosteric inhibitor of K-Ras(G12D), binds to K-Ras(G12D) P110 site with KD of 88 uM in MST assay; KAL-21404358 disrupts the K-RasG12D-B-Raf interaction using a NanoBiT split luciferase assay, and to impair the Raf-MEK-ERK and the PI3K-AKT signaling pathways. KAL-21404358 exhibited specificity for K-RasG12D over K-RasWT, H-RasWT, Rap1a, R-Ras and R-Ras2.
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DC70730 Ras binder 2C07 Featured
Ras binder 2C07 is a switch-II binding ligand which binds Ras GDP and GTP states.
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DC74365 RMC-4998 Featured
RMC-4998 (RMC4998) is a tricomplex inhibitor that targets the active state or GTP-bound state of KRAS G12C, selectively inhibits the proliferation of KRASG12C mutant cells with mean IC50 of 0.28 nM.
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DC42419 Antineoplaston A10 Featured
Antineoplaston A10 is a naturally occurring substance in the human body that that can be potentially used for the treatment of glioma, lymphoma, astrocytoma and breast cancer. The main ingredient active of antineoplaston A10 (Phenylacetylglutamine, PG) inhibits RAS and promotes apoptosis.
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DC74574 LY3537982 (KRAS G12C inhibitor 19)
LY3537982 (KRAS G12C inhibitor 19) is a highly selective and potent inhibitor of the  KRAS-G12C protein. LY3537982 selectively inhibits the growth of KRAS G12C mutant cells H23 G12C, H358 G12C, and H2122 G12C with IC50s of 1.04 nM, 1.16 nM, and 11.38 nM, respectively.
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DC74369 SIJ1795
SIJ1795 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 82 and 75 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.
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DC74368 SIJ1772
SIJ1772 is a potent mutated RAS (mtRAS)-signaling pathway blocker/inhibitor with IC50 of 77 and 96 nM for Ba/F3-NRAS-G12D and Ba/F3-NRAS-G12V, respectively.
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DC74367 SCH53239
SCH-53239 (SCH53239) is a small molecule inhibitor of Ras nucleotide exchange with IC50 of 0.5 uM, bind competitively with GDP in the nucleotide binding site of the Ras protein.
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DC74366 RSC-1255
RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity.
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DC74364 G12Si-5
G12Si-5 is a specific small molecule that covalently target K-Ras(G12S) mutation, suppresses K-Ras(G12S) signaling, preferentially inhibits the growth of the K-Ras(G12S)-transduced cells with IC50 of 2.4 uM.
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DC74363 Fulzerasib
Fulzerasib is a potent selective inhibitor of KRAS gene mutation.
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DC74362 ERAS-5024
ERAS-5024 (ERAS5024) is a potent and selective KRAS G12D inhibitor with IC50 of 0.86 nM in RAS-RAF binding assays, inhibits ERK1/2 phosphorylation (pERK) formation with IC50 of 2.1 nM in AsPC-1 cell-based assays.
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DC74361 CSC01
CSC01 is a small molecule inhibitor of oncogenic KRAS mutant G13D (KRAS-G13D).
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DC74359 BBO-8956
BBO-8956 is a highly potent, covalent inhibitor of GTP-KRAS G12C, BBO-8956 is effective against both GDP and GTP-bound KRAS G12C.
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DC74358 ASP6918
ASP6918 (ASP 6918) is a highly potent, covalent KRAS G12C inhibitor with IC50 of 28 nM in cell-free assays, and pERK inhibition IC50 of 3.7 nM in NCI-H1373 cells.
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DC74357 ADT-007
ADT-007 (ADT007) is a potent, specific pan-RAS inhibitor, shows potential to circumvent resistance to mutant-specific KRAS inhibitors and activates antitumor immunity.
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DC74356 ACA22
ACA22 is a small molecule KRAS inhibitor, inhibits KRAS-mediated signal transduction in cells expressing wild type (WT) and G12D mutant KRAS.
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DC74355 ACA-14
ACA-14 is a small molecule direct inhibitor of KRAS, impedes the interaction of KRAS with its effector Raf and reduces both intrinsic and SOS-mediated nucleotide exchange rates.
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DC74354 6H05 trifluoroacetate
6H05 is a selective, allosteric inhibitor of oncogenic mutant K-Ras(G12C), an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors..
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DC74353 1-AM
A potent, selective, covalent KRAS G12C inhibitor that selectively inhibit KRAS G12C-dependent signaling and cancer cell growth at sub-micromolar concentrations..
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DC10949 RasGRP3 ligand 96 Featured
RasGRP3 ligand 96 is a potent, selective ligand of Ras guanine-releasing protein 3 (RasGRP3) with Ki of 1.75 nM, showed 73-fold and 45-fold selectivity relative to PKCα and PKCε for in vitro binding activity resepctively.
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DC12031 ARS-1630 Featured
ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound..
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DC10738 ARS-1323 Featured
ARS-1323 is a novel inhibitor of mutant K-ras G12C.
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DC70578 LY-3537982 Featured
LY-3537982 (LY3537982) is a highly selective and potent KRAS-G12C inhibitor, selectively inhibits growth of KRAS G12C mutant cells (IC50=1-60 nM).LY-3537982 does not inhibit growth of KRAS G12S/G13C/G12D mutant cells and WT KRAS cells (CI50>10 uM).LY-3537982 displays high selectivity for proteome-wide cysteine residues was evaluated using competitive chemical proteomics (8866 peptides).LY3537982 inhibits the growth of subcutaneous EL3187 NSCLC PDX tumors in nude mice in a dose dependent manner.LY3537982 demonstrates robust tumor regression in combination with other agents in KRAS G12C in vivo models.LY3537982 is a promising KRAS G12C inhibitor predicted to deliver >90% KRAS G12C target occupancy in the clinic.
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DC70046 MRTX 0902 Featured
MRTX0902 is a potent SOS1 inhibitor with an IC50 of 46 nM (WO2021127429A1; Example 12-10).
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DC47210 JDQ-443 Featured
JDQ443 (example 1a) is a covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1).
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DC70234 AZD4625 Featured
AZD4625 is a potent, selective, covalent allosteric inhibitor of mutant GTPase KRAS G12C with IC50 of 3 nM, inhibitor H358 cell proliferation with GI50 of 4 nM.AZD4625 is a clinical development candidate for the treatment of KRASG12C positive tumors.
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DC47351 ASP2453 Featured
ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC50 value of 40 nM.
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