Catalog No.
Product Name
Application
Product Information
Citations
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KRAS Inhibitor
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. -
KRAS Inhibitor
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. -
KRAS G12D Inhibitor
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. -
KRASG12D PROTAC Degrader
PROTAC K-Ras Degrader-5 is a cereblon-based PROTAC specifically designed to target KRASG12D, achieving a DC50 of less than 100 nM. This reagent facilitates the recruitment of KRASG12D to the cereblon E3 ubiquitin ligase complex, leading to its ubiquitination and proteasomal degradation. As a result, it effectively reduces pERK levels and inhibits the proliferation of cancer cells. PROTAC K-Ras Degrader-5 also enhances caspase 3/7 activity and cleaved PARP levels, indicative of apoptosis, in pancreatic cancer models. This compound is a valuable tool for researching both pancreatic and colorectal cancer. -
KRAS G12C Inhibitor
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. -
KRas G12V Inhibitor
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. -
KRAS G12C Inhibitor
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. -
KRAS(Q61H) Inhibitor
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. -
KRAS G12D Inhibitor
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. -
KRASG12C Inhibitor
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. -
KRAS Inhibitor
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. -
KRAS G12D Inhibitor
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. -
KRAS Inhibitor
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. -
KRASG12C Inhibitor
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. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a dissociation constant (KD) of 203 pM. This compound effectively disrupts the function of the KRas signaling pathway, making it a valuable tool for investigating tumor biology and related therapeutic strategies. Deltasonamide 1 holds promise for advancing research in cancer treatment and understanding related pathophysiological mechanisms. -
KRAS Inhibitor
Deltarasin hydrochloride is a potent inhibitor of the interaction between KRAS and PDEδ, exhibiting a binding affinity (Kd) of 38 nM for purified PDEδ. This compound is crucial for research applications focused on targeting KRAS-driven oncogenesis, primarily in cancer studies. By disrupting this interaction, Deltarasin hydrochloride facilitates investigations into therapeutic strategies aimed at KRAS mutations and their downstream signaling pathways. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 TFA is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a binding affinity with a KD of 203 pM. This compound is valuable in research focused on cancer biology, particularly in the study of tumor progression and metastasis. Its ability to disrupt the PDE6δ-KRas axis makes it a useful tool for investigating the underlying mechanisms of KRas-driven malignancies. -
KRAS G12C Inhibitor
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. -
RAS/RAS-RAF Inhibitor
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. -
Ras-Raf Inhibitor
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. -
pan-KRAS PROTAC Degrader
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment. -
KRAS-PDEδ Inhibitor
NHTD is a selective inhibitor of KRAS-PDEδ, targeting the prenyl-binding pocket of PDEδ and modulating the cellular localization of KRAS. This action effectively inhibits the proliferation of KRAS-mutant cancer cells and promotes apoptosis. NHTD is a valuable tool for investigations into KRAS-driven non-small cell lung cancer (NSCLC) and related oncology research. -
KRAS Inhibitor
KRAS-IN-56 is a selective KRAS inhibitor that targets the interaction between GTP-bound KRAS and SOS1, demonstrating an EC50 of 33 μM. This compound effectively reduces phosphorylated ERK (p-ERK) levels, making it a valuable tool for studying MAPK signaling pathways. KRAS-IN-56 is particularly relevant for research applications involving lung cancer and other KRAS-driven malignancies. -
KRAS G12C Inhibitor
KRAS G12C inhibitor 27 is a potent inhibitor targeting the KRAS G12C mutant protein, which plays a pivotal role in various cancers. This compound exhibits significant antitumor activity, making it a valuable tool for research in cancer biology and therapeutic development. Its application extends to studying KRAS-driven tumors and evaluating the efficacy of targeted therapies. -
KRAS G12D Inhibitor
KRAS G12D inhibitor 3 is a selective inhibitor targeting the KRAS G12D mutant with an IC50 of less than 500 nM. It exhibits significant antitumor activity, making it relevant for cancer research focused on KRAS-driven tumors. Additionally, this compound functions as a click chemistry reagent, featuring an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition with azide-containing molecules, facilitating various bioconjugation applications in molecular biology. -
G12Si-1 Analog
G12Si-2 is an analog of G12Si-1 that serves as a negative control in research applications. It acts as a non-covalent inhibitor specifically for the G12S mutant of K-Ras. This compound is valuable for studies aimed at elucidating the mechanisms of K-Ras signaling and evaluating the effects of various inhibitors in cellular contexts. -
KRAS G12C Inhibitor
KRAS G12C-IN-74 is a selective inhibitor of KRAS G12C with a target IC50 of 43.18 nM. This compound induces G0/G1 cell cycle arrest and promotes apoptosis specifically in KRAS G12C-mutated cancer cells. It is suitable for research applications focusing on KRAS G12C-driven pancreatic, colorectal, and lung cancers. -
cAMP Analogue
8-CPT-cAMP-AM is a membrane-permeant analogue of cyclic adenosine monophosphate (cAMP) that acts as an activator of cAMP- and cGMP-dependent protein kinases. It also stimulates exchange protein directly activated by cAMP (Epac), making it a valuable tool for investigating cAMP signaling pathways. This compound is useful in research applications studying cellular processes influenced by cAMP, such as cell proliferation, differentiation, and effects on various physiological responses. -
pan-KRAS Inhibitor
pan-KRAS-IN-6 is a highly potent pan-KRAS inhibitor, exhibiting IC50 values of 9.79 nM for Kras G12D and 6.03 nM for Kras G12V. This compound effectively targets KRAS mutant forms associated with various cancers, making it a valuable tool for studying KRAS signaling pathways and evaluating therapeutic strategies in KRAS-driven tumors. Its specificity and efficacy position it as a key reagent in cancer research and drug discovery efforts targeting KRAS-related malignancies. -
KRAS G12C inhibitor
KRAS G12C inhibitor 21 is a selective inhibitor targeting the KRAS G12C oncogene. It effectively disrupts downstream signaling pathways associated with cell proliferation and survival in KRAS-driven malignancies. This compound is primarily utilized in cancer research to explore therapeutic strategies for malignancies harboring KRAS G12C mutations. -
Anti-cancer Agent
KRAS G12C inhibitor 37 is a selective inhibitor targeting the KRAS G12C mutation, a key driver in various cancers. This compound displays significant efficacy in disrupting KRAS-mediated signaling pathways, thus impeding tumor growth and proliferation. KRAS G12C inhibitor 37 is intended for research applications focused on elucidating the therapeutic potential in KRAS G12C-driven malignancies. -
pan-KRAS Inhibitor
pan-KRAS-IN-15 is a pan-KRAS inhibitor that targets multiple KRAS mutant variants. This compound exhibits potent inhibitory activity against KRAS-driven signaling pathways, making it valuable for studying the mechanisms of KRAS-related cancers. It is particularly relevant for research focused on pancreatic cancer, providing insights into therapeutic strategies and disease progression. -
KRAS Inhibitor
KRAS Inhibitor-22 is a selective inhibitor of the K-Ras protein, specifically targeting the Kras 4B(G12D) and Kras 4B(G12C) mutant forms. This compound exhibits potent anti-cancer activity, making it a valuable tool in cancer research aimed at understanding K-Ras-driven malignancies. Its application can aid in elucidating the role of K-Ras in cancer progression and therapeutic resistance. -
KRAS G12C Inhibitor
KRAS inhibitor-13 is a selective inhibitor targeting the mutant KRAS G12C protein, demonstrating its potency with an IC50 value of 0.883 µM. This compound effectively inhibits phosphorylated ERK (p-ERK) in cell lines, showing IC50s of 5.9 µM in MIA PaCA-2 cells and >100 µM in A549 cells. KRAS inhibitor-13 is poised for research applications focused on pancreatic, colorectal, and lung cancers, providing insights into therapeutic strategies against KRAS-driven malignancies. -
KRAS G12C Inhibitor
KRAS G12C Inhibitor 44 is a potent and orally bioavailable inhibitor targeting the KRAS G12C mutation. This compound exhibits significant anti-proliferative activity, with IC50 values of 0.016 µM in MIA PaCA-2 cells and 0.028 µM in H358 cells. Additionally, KRAS G12C Inhibitor 44 demonstrates antitumor effects in vivo, making it a valuable tool for cancer research focusing on KRAS-driven malignancies. -
KRAS G12C Inhibitor
KRAS G12C inhibitor 52 is a selective inhibitor targeting the KRAS G12C mutant protein. This compound effectively disrupts KRAS signaling pathways, thereby inhibiting cell proliferation and survival in KRAS G12C-driven cancers. Its research applications include studies on cancer biology, drug development, and understanding resistance mechanisms in targeted therapies. -
KRAS G12C Inhibitor
KRAS inhibitor-12 is a potent inhibitor specifically targeting the KRAS G12C mutation, exhibiting an IC50 of 0.537 µM. This compound demonstrates effective inhibition of phosphorylated ERK in MIA PaCA-2 and A549 cells, with IC50 values of 1.3 µM and 3.7 µM, respectively. KRAS inhibitor-12 is a valuable tool for investigating therapeutic strategies in pancreatic, colorectal, and lung cancers. -
Anti-cancer Agent
KRAS G12D inhibitor 12 specifically targets the KRAS G12D mutation, a critical player in cellular signaling pathways associated with tumorigenesis. This compound exhibits potent anti-cancer activity, making it a valuable tool for researchers investigating KRAS G12D-mediated cancers. Its application includes evaluating therapeutic strategies and understanding the molecular mechanisms of oncogenic signaling in various cancer types. -
KRAS G12C Inhibitor
KRAS G12C Inhibitor 46 is a potent inhibitor targeting the KRAS G12C mutation, an essential driver in various cancers. This compound effectively blocks the aberrant signaling pathways associated with KRAS G12C, leading to reduced proliferation and enhanced apoptosis in cancer cells harboring this mutation. It is primarily utilized in cancer research, particularly for exploring therapeutic strategies targeting KRAS-dependent tumors. -
KRAS Inhibitor
KRAS Inhibitor-23 is a selective inhibitor targeting KRAS, a critical protein involved in cell signaling pathways that regulate cell growth and differentiation. This compound demonstrates significant biological activity by effectively disrupting KRAS-mediated oncogenic signaling, making it a valuable tool in cancer research. Its application spans the investigation of KRAS mutations and their role in tumor progression, providing insights into potential therapeutic strategies for KRAS-driven malignancies. -
KRASG12D Inhibitor
KRASG12D-IN-5 is a potent inhibitor targeting the KRAS(G12D) mutation, exhibiting an IC50 of 11 nM. This compound demonstrates significant anticancer activity, displaying low cytotoxicity against various cell lines, including 10.37 μM for BxPC-3 (wild type), 0.76 μM for KRAS mutant AsPC-1 (G12D), and 0.3 μM for MIAPaCa-2 (G12C). KRASG12D-IN-5 is valuable for cancer research, particularly in the context of lung, pancreatic, and colorectal cancers. -
Mutant KRAS Inhibitor
KRAS-IN-48 free base is a highly selective inhibitor targeting mutant KRAS, specifically KRAS G12D and KRAS G12V, with Kd values of 2.58 nM and 5.49 μM, respectively. This compound effectively reduces pERK expression in KRAS-mutant cells, exhibiting IC50 values of 1.1 μM and 1.51 μM for KRAS G12D and G12V mutations. KRAS-IN-48 free base serves as a valuable tool in cancer research, contributing to the understanding of KRAS-driven malignancies. -
KRAS G12D Inhibitor
KRAS G12D inhibitor 24 is a potent inhibitor of the KRAS G12D mutant, exhibiting an IC50 of 0.004 μM. This compound demonstrates significant oral bioactivity, making it suitable for in vivo studies. Its primary applications include exploring therapeutic avenues in cancer research, specifically for tumors driven by KRAS G12D mutations. -
KRAS G12C Inhibitor
KRAS G12C inhibitor 58 specifically targets the KRAS G12C mutant protein, effectively disrupting its activity and downstream signaling pathways. This compound demonstrates potent antitumor efficacy, making it a valuable tool for studying KRAS-driven malignancies. Its applications extend to cancer research, particularly in the development and testing of novel therapeutic strategies for treating KRAS G12C-dependent tumors. -
KRAS Inhibitor
pan-KRAS-IN-13 is a potent KRAS inhibitor that targets mutant forms of the KRAS protein, demonstrating IC50 values of 2.75 nM and 2.89 nM for G12D and G12V mutations, respectively. This compound is valuable for research applications aimed at understanding KRAS-driven cancers and evaluating therapeutic strategies to inhibit KRAS signaling pathways. Its high specificity and efficacy make it a critical tool for the study of oncogenic mutations associated with various malignancies. -
KRAS G12D Inhibitor
RNK08954 is a KRAS G12D inhibitor targeting the KRAS oncogene mutation commonly found in various cancers. This compound demonstrates the ability to impede KRAS-driven cellular signaling pathways, making it a valuable tool for investigating the role of KRAS G12D in tumorigenesis. RNK08954 is suitable for research applications focused on cancer biology and therapeutic development against KRAS-mutant tumors. -
cAMP Analogue
8-Br-2'-O-Me-cAMP is a synthetic analog of cyclic AMP (cAMP) that selectively activates exchange factors activated by cAMP (Epac) without stimulating protein kinase A (PKA). This unique property makes it a valuable tool for investigating cAMP-mediated signaling pathways. It is particularly relevant in studies related to cardiovascular diseases, facilitating the exploration of Epac's role in cardiac function and pathology. -
Anti-cancer Agent
KRAS G12C inhibitor 40 is a selective inhibitor targeting the KRAS G12C mutation, a critical driver in various cancers. This compound disrupts the aberrant signaling pathways associated with KRAS G12C, demonstrating significant anti-cancer activity. KRAS G12C inhibitor 40 is valuable for research into the mechanisms of KRAS G12C-mediated tumorigenesis and for the development of targeted cancer therapies. -
KRAS G12C Inhibitor
ARS-2102 is a potent covalent inhibitor of the KRAS G12C mutation, a key driver in various cancers. By selectively targeting this mutated oncogene, ARS-2102 exhibits significant anti-tumor activity, making it a valuable tool for cancer research. Its application is particularly relevant in studies focused on therapeutic strategies for KRAS-driven malignancies. -
Rce1 Inhibitor
NSC 1008 is a selective inhibitor of Ras converting enzyme 1 (Rce1), exhibiting an in vitro IC50 of 8.9 μM in human cells. This compound demonstrates specificity for Rce1, showing minimal inhibitory effects on human Ste24 and farnesyltransferase. NSC 1008 has low cellular toxicity and effectively induces mislocalization of EGFP-Ras from the plasma membrane in cancer cells. It serves as a valuable reagent for cancer research, facilitating studies on Rce1's role in oncogenic signaling pathways.
