Ras

Cat. No.

A25638

CAS No.

2446485-15-8

SHY-855

SHY-855 is a pan-Ras inhibitor that selectively targets K-Ras and other members of the Ras superfamily of small GTPases, with IC50 values ranging from 0.3 to 5 μM. This compound effectively inhibits the phosphorylation of key downstream signaling molecules, including MEK, ERK1/2, and AKT, thereby disrupting Ras-GTP activity complex formation. SHY-855 is suitable for research applications focused on pancreatic cancer and non-small cell lung cancer, facilitating studies on Ras-mediated signaling pathways.

Cat. No.

A25780

CAS No.

2446484-96-2

SHY-867

SHY-867 is a pan-Ras inhibitor that prevents the binding of K-Ras proteins and other members of the Ras superfamily of small GTPases, exhibiting EC50 values between 0.5-3 μM. This compound effectively inhibits the phosphorylation of critical downstream signaling molecules, including MEK, ERK1/2, and AKT. SHY-867 is a valuable tool for research applications focusing on pancreatic cancer and non-small cell lung cancer, facilitating investigations into Ras-GTP activity and related molecular pathways.

Cat. No.

A25823

CAS No.

3060515-08-1

YK-8S

YK-8S is a dual-targeted covalent inhibitor of K-Ras mutations G12D and G12C. This compound demonstrates selective binding, showing minimal affinity for wild-type K-Ras and other mutants. YK-8S exhibits significant anti-proliferative effects on H358 (G12C) and AGS (G12D) cancer cell lines, and effectively inhibits downstream signaling by reducing p-AKT and p-ERK phosphorylation in BaF3 cells harboring the G12D and G12C mutations. It is a valuable reagent for research on pancreatic and colorectal cancers characterized by high incidences of the G12D mutation.

Cat. No.

A25852

CAS No.

3027172-23-9

pan-KRAS-IN-5

pan-KRAS-IN-5 is a pan-KRAS inhibitor that functions by targeting 5′-UTR RNA G-quadruplexes (rG4s). It effectively binds to and stabilizes KRAS rG4s, leading to the inhibition of KRAS translation and downstream signaling via the MAPK and PI3K-AKT pathways. This compound has been shown to induce cell cycle arrest and promote apoptosis in KRAS-driven cancer cells, while also inhibiting tumor growth and KRAS expression in KRAS-mutant xenograft models. pan-KRAS-IN-5 is suitable for investigations into KRAS-related oncogenesis and therapeutic strategies for KRAS-driven cancers.

Cat. No.

A25931

CAS No.

694515-65-6

Rac1-IN-5

Rac1-IN-5 is a potent and reversible inhibitor of the RAC1 protein, with a binding affinity (KD) of 30 nM. It functions by competing with guanine nucleotides for the binding site on RAC proteins, thereby effectively inhibiting RAC1 activity and associated cellular functions. This compound demonstrates significant anti-tumor metastatic properties in vivo and has the potential to enhance survival rates. Rac1-IN-5 is valuable for investigating invasive cancers, including triple-negative breast cancer and colon cancer.

Cat. No.

A25934

CAS No.

3055319-82-6

VVD-699

VVD-699 is a covalent inhibitor targeting the RAS-p110α interaction, demonstrating oral bioavailability. It effectively inhibits the activation of PI3Kα with an IC50 of 104 nM in H358 cells and reduces phosphorylated AKT levels. This compound is relevant for research into KRAS mutant and amplified cancers, providing insights into potential therapeutic strategies.

Cat. No.

A28727

CAS No.

2768099-61-0

KRAS G12D inhibitor 25

KRAS G12D inhibitor 25 selectively targets the KRAS G12D mutation and HSP90α, exhibiting IC50 values of less than 0.1 μM and between 0.1-1 μM, respectively. This compound effectively inhibits the proliferation of MIA PaCa-2 and NCI-H358 cell lines, displaying EC50 values of less than 0.1 μM and between 0.1-1 μM, respectively. Additionally, KRAS G12D inhibitor 25 promotes the degradation of ERBB2 with a DC50 range of 0.1-1 μM, making it a valuable tool for cancer research focusing on KRAS-targeted therapies.

Cat. No.

A30497

CAS No.

300809-71-6

KRAS inhibitor-9

KRAS inhibitor-9 is a selective inhibitor of the KRAS protein, primarily targeting KRAS G12D, G12C, and Q61H mutations with a moderate binding affinity (Kd=92 μM). This compound effectively disrupts the formation of the GTP-bound active form of KRAS, leading to subsequent inactivation of downstream signaling pathways. Biological assays demonstrate that KRAS inhibitor-9 induces G2/M cell cycle arrest and promotes apoptosis in non-small cell lung cancer (NSCLC) cells harboring KRAS mutations, while sparing normal lung cells. Its application is significant in cancer research, particularly in studying KRAS-driven malignancies.

Cat. No.

A30869

CAS No.

2765254-39-3

KRAS G12D inhibitor 14

KRAS G12D inhibitor 14 is a selective inhibitor targeting the KRAS G12D mutation, exhibiting a binding affinity (KD) of 33 nM. This compound effectively reduces the levels of active KRAS G12D (KRAS G12D-GTP) without impacting the KRAS G13D variant. It is a valuable tool for research applications focused on elucidating the role of KRAS G12D in oncogenic signaling pathways and developing targeted cancer therapies.

Cat. No.

A31715

CAS No.

865784-65-2

Antitumor agent-60

Antitumor agent-60 is a potent inhibitor of the RAS-RAF signaling pathway, specifically binding to CRAF with a Kd value of 3.93 μM. This compound induces apoptosis by arresting the cell cycle at the G2/M phase and elevates p53 levels and reactive oxygen species (ROS) within cells. Additionally, antitumor agent-60 induces morphological changes, including oval and irregular nuclei in cancer cells. In vivo studies demonstrate its ability to suppress tumor growth in an A549 xenograft model, underscoring its potential for cancer research applications.

Cat. No.

A36283

CAS No.

3029443-36-2

BBO-11818

BBO-11818 is a highly selective non-covalent pan-KRAS inhibitor, targeting the Switch-II/Helix 3 pocket with an IC50 range of 28-120 nM. This compound effectively disrupts the KRAS:RAF1 interaction, leading to inhibition of the MAPK signaling pathway, resulting in significant anti-tumor effects. It demonstrates the ability to not only inhibit cell proliferation and induce apoptosis but also promote tumor regression in xenograft models. BBO-11818 is particularly valuable in research focused on KRAS mutation-related malignancies, including pancreatic cancer, non-small cell lung cancer, and colorectal cancer, and exhibits synergistic effects when used in combination with other therapeutic agents.

Cat. No.

A36628

CAS No.

3022287-75-5

KRAS G12D-IN-30

KRAS G12D-IN-30 is a selective inhibitor of the KRAS G12D mutant, targeting the KRAS oncogene involved in various cancers. By inhibiting the activation of the downstream MAPK signaling cascade, specifically the Raf1-MEK-ERK pathway, this compound provides valuable insights into oncogenic signaling mechanisms. KRAS G12D-IN-30 is suitable for cancer research applications, particularly in studies focusing on KRAS-driven tumor biology and therapeutic strategies.

Cat. No.

A36673

CAS No.

3033690-83-1

KRAS inhibitor-27

KRAS inhibitor-27 is a specific inhibitor targeting KRAS mutations, particularly effective against KRAS G12D and G12V variants. It demonstrates potent biological activity with IC50 values of 378 nM and 0.6 nM in AsPC-1 and SW620 cell lines, respectively, while showing a markedly reduced effect on wildtype KRAS HT-29 cells (IC50 3230 nM). This compound effectively inhibits ERK phosphorylation and reduces DUSP4 expression, thereby disrupting the MAPK signaling pathway. KRAS inhibitor-27 is valuable for research applications focusing on cancer biology and therapeutic strategies against KRAS-driven tumors.

Cat. No.

A36712

CAS No.

3023465-61-1

KRAS G12C-IN-76

KRAS G12C-IN-76 is a selective inhibitor of the KRAS G12C mutation, a prominent driver in various cancers. This compound effectively reduces ERK phosphorylation, thereby impeding signaling pathways involved in tumor growth and proliferation. KRAS G12C-IN-76 demonstrates significant anti-cancer activity, particularly in pancreatic cancer models, making it a valuable tool for research in targeted therapies and cancer biology.

Cat. No.

A36738

CAS No.

3076211-50-9

KRAS-IN-51

KRAS-IN-51 is a selective inhibitor of the KRas G12V mutant, exhibiting an IC50 of 2.9 nM. It demonstrates effective inhibition of pERK phosphorylation and shows significant anti-proliferative activity in colorectal cancer (SW620) and pancreatic cancer (MIAPaCa-2) cell lines. This compound is valuable for research focused on KRas-driven malignancies, contributing to the understanding of therapeutic strategies targeting KRas mutations.

Cat. No.

A36749

CAS No.

2300967-40-0

KRAS G12C inhibitor 61

KRAS G12C Inhibitor 61 is a selective inhibitor targeting the KRAS G12C mutation. It effectively inhibits phospho-ERK 1/2 in MIA PaCa-2 cells, exhibiting an IC50 of 9 nM. This compound is valuable for research into pancreatic, colorectal, and lung cancers, contributing to studies focused on therapeutic strategies for KRAS-driven malignancies.

Cat. No.

A36753

CAS No.

3058972-05-4

RM-046

RM-046 is a selective inhibitor targeting the KRAS(Q61H) mutant, functioning through the formation of a ternary complex with cyclophilin A. This compound non-covalently binds to activated KRASQ61H, obstructing effector binding and thereby inhibiting downstream signal transduction pathways. RM-046 has demonstrated efficacy in suppressing ERK phosphorylation, stalling cancer cell proliferation, and promoting anti-tumor activity, including tumor regression in preclinical xenograft studies. It serves as a valuable tool for investigating KRASQ61H-associated malignancies.

Cat. No.

A36763

CAS No.

2938179-13-4

KRAS G12D-IN-27

KRAS G12D-IN-27 is a selective inhibitor targeting the KRAS G12D mutant protein. It effectively inhibits ERK phosphorylation, exhibiting an IC50 of 112 nM. This compound is valuable for cancer research, particularly in studies focused on the KRAS signaling pathway and downstream effects in tumor biology.

Cat. No.

A36774

CAS No.

2768868-14-8

KRASG12C IN-15

KRASG12C IN-15 is a potent inhibitor of the KRASG12C mutation, functioning primarily by obstructing the SOS1-mediated GDP/GTP exchange, with an IC50 of 19 nM. It effectively inhibits ERK phosphorylation with an IC50 of 0.051 μM and demonstrates significant anti-proliferative effects on KRASG12C-mutated MIA PaCa-2 cells, with an IC50 of 0.023 μM. In vivo studies reveal that KRASG12C IN-15 exhibits notable antitumor efficacy in MIA PaCa-2 xenograft mouse models. This compound is valuable for investigating KRASG12C-associated signaling pathways and developing targeted therapies.

Cat. No.

A37132

CAS No.

2922732-38-3

RMC-9945

Synonyms: RM-044

RMC-9945 is a selective, covalent inhibitor targeting the RAS(ON) G12D mutant form of KRAS. This orally active compound enhances β-Catenin/TCF transcriptional activity and demonstrates sustained disease control in preclinical models of colorectal cancer with early liver metastasis. RMC-9945 serves as a valuable tool for researching RAS-driven cancer mechanisms and potential therapeutic interventions.

Cat. No.

A39217

CAS No.

2915282-32-3

KRASG12C IN-19

KRASG12C IN-19 is a selective inhibitor that targets the KRASG12C mutation. It demonstrates potent antiproliferative effects against KRASG12C-mutant non-small cell lung cancer (NSCLC) cell line H358, with an IC50 of 7.6 nM, and effectively inhibits downstream ERK phosphorylation (IC50 = 24.06 nM). KRASG12C IN-19 shows minimal inhibitory activity against KRASG12V and KRASG12D mutants, with IC50 values exceeding 10,000 nM. This reagent forms a covalent bond with KRASG12V-GDP and provides a robust tool for research on KRASG12C-driven malignancies, including NSCLC, pancreatic cancer, and colorectal cancer.

Cat. No.

A39522

CAS No.

1054549-73-3

6-CEPN

6-CEPN is a potent inhibitor of RAS, acting by binding to isovalerylcysteine carboxymethyltransferase (Icmt) binding sites to effectively inhibit RAS activation. This compound exhibits significant anticancer properties by blocking the progression of cancer cells in the G1 phase of the cell cycle. Additionally, 6-CEPN promotes autophagy and necrosis in cancer cells, making it a valuable tool for research in cancer biology and therapeutic development.

Cat. No.

A40694

CAS No.

2447039-81-6

RAS/RAS-RAF-IN-1

RAS/RAS-RAF-IN-1 is a potent inhibitor targeting the RAS and RAS-RAF signaling pathways. With a dissociation constant (KD) in the range of 5.0 μM to 15 μM for cyclophilin A (CYPA), this compound demonstrates significant binding affinity. RAS/RAS-RAF-IN-1 exhibits notable antitumor activity, making it a valuable tool for cancer research and therapeutic development.

Cat. No.

A40701

CAS No.

1782098-79-6

Cyclorasin 9A5

Cyclorasin 9A5 is an 11-residue cyclic peptide that acts as an orthosteric inhibitor of the Ras-Raf protein interaction, exhibiting an IC50 of 120 nM. This compound is valuable for studying the Ras signaling pathway's involvement in various cancers and cellular processes. Its cell-permeable nature allows for effective in vitro and in vivo applications in cancer research and drug development targeting Ras-dependent pathways.

Cat. No.

A40854

CAS No.

3023465-20-2

KRAS G12C-IN-78

KRAS G12C-IN-78 is a selective inhibitor targeting the KRAS G12C mutant protein, binding to both inactive and active states. This compound effectively inhibits ERK1/2 phosphorylation and promotes covalent adduct formation with endogenous KRAS G12C, leading to the suppression of MAPK pathway gene expression and reduced cellular proliferation in KRAS G12C mutant cells. KRAS G12C-IN-78 is suitable for studying KRAS G12C mutant solid tumors, such as pancreatic ductal adenocarcinoma and non-small cell lung cancer.