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Catalog No.
Product Name
Application
Product Information
Citations
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Rac family GTPase inhibitor
EHT 1864 is an antiproliferative chemical shown to inhibit Rac family GTPases.- Natalie J Jooss, .et al. , J Thromb Haemost, 2023, Aug;21(8):2260-2267 PMID: 37150294
- Kakoki M, .et al. , JCI Insight, 2019, Jun 20;4(12) PMID: 31217360
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Cdc42 GTPase inhibitor
CASIN is a novel and potent Cdc42 inhibitor.- Yongru Xu, .et al. , Int J Mol Sci, 2017, Mar; 18(3): 586 PMID: 28282856
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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. -
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. -
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. -
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. -
Cdc42 Inhibitor
MLS-573151 is a selective inhibitor of the GTPase Cdc42, exhibiting an EC50 of 2 μM. It specifically targets Cdc42 without affecting other members of the GTPase family, such as Rab2, Rab7, H-Ras, Rac1, Rac2, and wild-type RhoA. By inhibiting GTP binding to Cdc42, MLS-573151 serves as a valuable tool for studying cellular processes regulated by this signaling pathway. Its application is essential in research related to cancer and other diseases where Cdc42 plays a critical role in cell migration and proliferation. -
Rac1 Inhibitor
Z62954982 is a selective Rac1 inhibitor with an IC50 of 12 μM, demonstrating notable potency in disrupting the Rac1/Tiam1 complex. This compound effectively reduces active Rac1 levels (GTP-bound) in the cytoplasm while preserving the function of other Rho GTPases such as Cdc42 and RhoA. Z62954982 serves as a valuable tool for studies investigating Rac1-mediated signaling pathways and their role in various biological processes. -
Tyrosinase Inhibitor
Norartocarpetin is a potent tyrosinase inhibitor, demonstrating significant inhibition with an IC50 value of 0.47 μM. This compound serves as an effective antibrowning agent for food systems research and exhibits notable anticancer activity against lung carcinoma cells (NCI-H460) with an IC50 of 22 μM. Its antiproliferative effects are mediated through targeting the Ras/Raf/MAPK signaling pathway, inducing mitochondrial-mediated apoptosis, causing S-phase cell cycle arrest, and inhibiting cell migration and invasion in human lung carcinoma cells. -
RAS-Effector PPI Inhibitor
RAS inhibitor Abd-7 is a selective RAS-binding compound (Kd=51 nM) that disrupts RAS-effector protein-protein interactions. This inhibitor effectively interferes with RAS-dependent signaling pathways by preventing the interactions between RAS and key effectors such as PI3K, CRAF, and RALGDS, as well as mutant KRAS proteins, NRAS Q61H, and HRAS G12V. RAS inhibitor Abd-7 is valuable for research applications targeting RAS-mediated processes in cancer biology. -
KRAS(G12C) Inhibitor
BBO-8520 is a selective covalent inhibitor of the KRAS G12C mutation, effectively promoting the inactive (OFF) state of KRAS by blocking GTP binding. This compound inhibits cell proliferation and disrupts the interaction between RAS and RAF1, leading to significant impact on oncogenic signaling pathways. BBO-8520 is suitable for research applications focusing on cancer biology and therapeutic strategies targeting KRAS-driven tumors. -
Rab27a-JFC1 Inhibitor
Nexinhib20 is a selective inhibitor of the Rab27a-JFC1 interaction (IC50: 2.6 μM) and Rac-1-GTP signaling. This compound effectively inhibits neutrophil exocytosis, adhesion, and β2 integrin activation, demonstrating significant anti-inflammatory properties. Nexinhib20 is suitable for research applications focused on systemic inflammation and myocardial ischemia-reperfusion injury. -
KRas Inhibitor
Pan KRas-IN-1 is a pan KRas inhibitor that targets mutant KRas proteins, particularly effective against KRas G12C inhibitor-resistant cancer models. It exhibits potent anti-cancer activity by disrupting KRas signaling pathways, thereby inhibiting tumor cell proliferation and survival. This compound is valuable in research applications focused on overcoming resistance mechanisms in KRas-driven malignancies. -
Cdc42 GTPase Inhibitor
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines. -
HIF-1α inhibitor
PRLX-93936 dihydrochloride (Compound 16) is a small-molecule inhibitor of hypoxia-inducible factor 1α (HIF-1α) with demonstrated anticancer activity. It also suppresses signaling within the activated Ras pathway, thereby inhibiting tumor cell proliferation and survival. PRLX-93936 shows potential therapeutic relevance in the study of relapsed or refractory multiple myeloma and other Ras-driven malignancies, making it a useful compound for investigating hypoxia-related and oncogenic signaling mechanisms in cancer. -
KRAS-G12C inhibitor
BI-0474 is a potent and selective inhibitor of the KRASG12C mutant, exhibiting an IC₅₀ of 7.0 nM for disruption of the GDP–KRAS::SOS1 protein–protein interaction. It demonstrates strong antiproliferative effects in NCI-H358 cells harboring the KRASG12C mutation and displays significant antitumor efficacy in non-small cell lung cancer (NSCLC) xenograft models. Through covalent targeting of mutant KRAS, BI-0474 effectively suppresses downstream MAPK signaling, making it a valuable compound for KRAS-driven cancer research and drug development. -
Epac1 Inhibitor
AM-001 is a non-competitive and selective inhibitor of Epac1 (exchange protein directly activated by cAMP 1). It blocks Epac1-mediated activation of the small GTPase Rap1 in cultured cells, thereby modulating cAMP-dependent signaling pathways independent of PKA. Through inhibition of Epac1–Rap1 signaling, AM-001 has shown potential for use in cardiovascular and heart disease research, particularly in studies exploring cardiac remodeling, hypertrophy, and fibrosis. -
MRTF-A/SRF Inhibitor
CCG-100602 is a selective small-molecule inhibitor of the myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling pathway. It specifically blocks the nuclear translocation of MRTF-A, thereby suppressing SRF-mediated transcriptional activity associated with fibrogenesis. Through this mechanism, CCG-100602 effectively downregulates profibrotic gene expression and serves as a valuable research tool for studying cytoskeletal dynamics, fibrosis, and transcriptional regulation. -
KRAS G12C inhibitor
Calderasib (MK-1084) is a highly selective inhibitor of the KRASG12C mutant, exhibiting potent antitumor activity in preclinical and clinical studies. By covalently binding to the cysteine residue within the mutant KRAS, Calderasib effectively suppresses downstream MAPK signaling and tumor cell proliferation. It can be employed as a monotherapy or in combination with immune checkpoint inhibitors such as pembrolizumab for oncology research, particularly in KRASG12C-driven cancers. -
Cdc42/Rac1 inhibitor
(R)-Ketorolac is an orally active inhibitor of the small GTPases Cdc42 and Rac1. It suppresses GTPase activity, thereby modulating signaling pathways involved in cytoskeletal dynamics and cell motility. Through this mechanism, (R)-Ketorolac alters ovarian cancer cell behaviors associated with invasion and metastasis and has been shown to alleviate cancer-associated cachexia. Its dual roles in inhibiting tumor progression and improving systemic cancer outcomes make it a promising agent for cancer research. -
GGPP synthase inhibitor
Digeranyl bisphosphonate (DGBP) is a potent inhibitor of geranylgeranyl pyrophosphate (GGPP) synthase, a key enzyme in the isoprenoid biosynthesis pathway. By blocking GGPP production, DGBP prevents the geranylgeranylation of small GTPases such as Rac1, thereby interfering with their membrane localization and downstream signaling. This mechanism makes DGBP a valuable tool compound for studying protein prenylation and related cellular processes, including cytoskeletal regulation and oncogenic signaling. -
KRASG12C inhibitor
AZD4747 is a potent and selective covalent inhibitor of the mutant GTPase KRASG12C. It exhibits excellent blood–brain barrier permeability and demonstrates strong antitumor potential in preclinical models of pancreatic and colorectal adenocarcinoma. By irreversibly binding to the cysteine residue within the KRASG12C mutant, AZD4747 effectively suppresses downstream MAPK signaling, leading to inhibition of tumor cell proliferation and survival. -
KRAS G12C inhibitor
Elisrasib (D3S-001) is an orally active KRAS^G12C inhibitor that potently inhibits the proliferation of KRAS^G12C-mutant H358 and MIA PaCa-2 cells, with IC₅₀ values of 0.6 nM and 0.44 nM, respectively. It demonstrates good metabolic stability in hepatocytes, liver microsomes, plasma, and whole blood across multiple species. Elisrasib also exhibits favorable pharmacokinetic properties and significant antitumor efficacy in mouse models. -
SOS1 inhibitor
SOS1-IN-11 is a potent small-molecule inhibitor of SOS1, exhibiting an IC₅₀ value of 30 nM. It is used in research to disrupt the SOS1–KRAS interaction and modulate RAS signaling pathways in cancer models.
