Catalog No.
Product Name
Application
Product Information
Citations
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osteoclastic bone resorption inhibitor
Zoledronic acid is a bisphosphonate which used to multiple myeloma and prostate cancer treament. - Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
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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. -
KRas G12C inhibitor
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1. -
Kras-G12C inhibitor
KRas G12C inhibitor 3 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1. -
Kras-G12C inhibitor
KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1. -
Ras/Raf/MEK inhibitor
Balamapimod, also known as MKI-822, is a Ras/Raf/MEK inhibitor. -
Kras-G12C inhibitor 1
KRas G12C inhibitor 1 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1. -
pan GTPase inhibitor
CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM. -
RhoA subfamily Rho GTPases inhibitor
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. -
Ras inhibitor
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer. -
Rho family GTPases inhibitor
MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. -
MRTF pathway inhibitor
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. -
S-IIP inhibitor/KRASG12C Probe
ARS-1323-Alkyne is a novel KRASG12C occupancy probe. -
KRAS G12D PROTAC Degrader
Setidegrasib is a PROTAC degrader specifically targeting the KRAS G12D mutation with a DC50 of 37 nM. This compound effectively induces the degradation of KRAS G12D protein, leading to the suppression of key signaling molecules such as p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates significant anti-tumor activity across various cancer xenograft models, making it a valuable tool for studying KRAS(G12D)-mutated solid tumors. -
KRAS degrader
ACBI3 is a PROTAC designed to target KRAS, employing a unique mechanism to induce degradation of this oncogenic protein. It comprises a pan-KRAS degrader linked to an E3 ligase ligand through a specialized linker, facilitating the recruitment of the proteasome for degradation. ACBI3 has demonstrated significant biological activity by achieving durable modulation of signaling pathways and promoting tumor regression in KRAS mutant xenograft mouse models, making it a valuable tool for research into cancer therapeutics aimed at KRAS-driven malignancies. -
PROTAC KRAS G12D Degrader
PROTAC KRAS G12D degrader 1 functions as a selective PROTAC targeting the KRAS G12D mutant by promoting its degradation. This compound effectively inhibits the proliferation of KRAS G12D-mutant cell lines and suppresses phosphorylation of ERK, a critical pathway in cancer signaling. In vivo studies demonstrate its ability to impede tumor growth in mice with AsPC-1 xenografts, making it a valuable tool for research into KRAS G12D-driven cancers. -
SOS1 Inhibitor
SOS1-IN-14 is a potent and selective inhibitor of SOS1, demonstrating an IC50 value of 3.9 nM. This orally active compound is absorbed in the intestine through a P-glycoprotein-mediated efflux mechanism. SOS1-IN-14 is primarily utilized in research on KRAS-mutated cancers, showcasing superior tumor suppression capabilities compared to alternative therapies. -
Rac1 Inhibitor
Rac1-IN-4 is a selective inhibitor of Rac1, a Rho GTPase involved in various cellular processes including cytoskeletal dynamics and cell migration. This compound effectively disrupts the signaling pathways mediated by Rac1, making it a valuable tool for studying cancer metastasis and neurodegenerative diseases. Rac1-IN-4 is utilized in research to explore the therapeutic potential of targeting Rac1 in cellular signaling and pathology. -
Ras Inhibitor
ASP2453 is a selective and orally bioavailable inhibitor targeting the KRAS G12C mutation. It functions by inhibiting the interaction between KRAS G12C and Raf mediated by Son of Sevenless (SOS), demonstrating an IC50 value of 40 nM. ASP2453 shows potential in cancer research, particularly in studies addressing KRAS-driven malignancies. -
K-Ras Inhibitor
KRpep-2d is a potent inhibitor of K-Ras, targeting the K-Ras signaling pathway known for its role in various cancers. This compound effectively reduces the proliferation of K-Ras-driven cancer cells, making it a valuable tool for cancer research. Its application can aid in the development of therapeutic strategies for K-Ras-associated malignancies. -
SOS1/KRAS Inhibitor
SAH-SOS1A TFA is a peptide-based inhibitor targeting the SOS1-KRAS protein interaction. It exhibits nanomolar affinity for both wild-type and various mutant KRAS forms, including G12D, G12V, G12C, G12S, and Q61H (EC50 = 106-175 nM). By directly disrupting nucleotide association, SAH-SOS1A TFA effectively impairs KRAS-driven cancer cell viability and inhibits the downstream ERK-MAPK phosphosignaling cascade, making it a valuable tool for research in cancer biology. -
SOS1 Inhibitor
SOS1-IN-15 is a potent SOS1 inhibitor with an IC50 value of 5 nM, designed to specifically target and inhibit SOS1 activity. Its strong inhibitory effect makes it a promising candidate for research into KRAS-driven cancers, facilitating the understanding of oncogenic signaling pathways and development of targeted therapeutic strategies. -
Anticancer Agent
ARN22089 is a novel trisubstituted pyrimidine that acts as an anticancer agent by inhibiting the interaction of CDC42 GTPases with downstream effectors. This mechanism disrupts critical signaling pathways involved in tumorigenesis. In preclinical studies, ARN22089 has demonstrated the ability to inhibit tumor growth in a BRAF mutant mouse melanoma model, making it a valuable compound for research in cancer therapeutics and signaling pathways. -
KRASG12C Inhibitor
RM-018 is a potent KRASG12C inhibitor that specifically targets the GTP-bound, active state of KRASG12C. This tricomplex compound effectively inhibits KRASG12C/Y96D, showcasing its potential to overcome resistance mechanisms. RM-018 is an invaluable tool for studying KRAS-related signaling pathways and developing targeted therapies in cancer research. -
NRAS Proto-oncogene Expression Reducer
RGB-1 is a selective RNA G-quadruplex stabilizer that targets and reduces the expression of the NRAS proto-oncogene within breast cancer cells. This compound serves as a valuable tool for exploring the cellular mechanisms and functions of RNA G-quadruplex structures, while also aiding in the identification of novel mRNA sequences capable of forming G-quadruplexes. RGB-1 is particularly relevant for research focused on breast cancer therapeutics and the molecular basis of oncogene regulation. -
Ras Activator
Methylophiopogonanone B is a homoisoflavonoid that serves as a Ras activator. Isolated from the root of Ophiopogon japonicus, it exhibits potent antioxidant properties. This compound enhances GTP-Rho levels and activates the Rho signaling pathway, thereby inducing morphological changes in cells, such as actin cytoskeletal reorganization, dendrite retraction, and stress fiber formation. It is a valuable reagent for research into cellular signaling and structural dynamics. -
Rac1/Cdc42 Inhibitor
AZA1 is a potent dual inhibitor of Rac1 and Cdc42, key regulators of cell signaling pathways. This compound has been shown to induce apoptosis in prostate cancer cells while simultaneously inhibiting their proliferation, migration, and invasion. AZA1 serves as a valuable tool for research into the molecular mechanisms of prostate cancer progression and potential therapeutic interventions.
