Ras Inhibitor

DCAI hydrochloride is a KRas inhibitor with a K_d value of 1.1 mM. DCAI hydrochloride directly binds to the Ras protein and competitively inhibits SOS-mediated nucleotide release (IC₅₀ = 155 μM) and exchange reaction (IC₅₀ = 342 μM). DCAI hydrochloride binds to the pocket at the Ras-SOS interface and blocks the formation of the Ras-SOS complex intermediate by impeding salt bridge formation through steric hindrance and the induction of Ras conformational changes. DCAI hydrochloride is used in the study of wild-type and mutant Ras tumors.

2C07 is a mutant Ras (K-Ras^M72C, H-Ras^M72C) inhibitor. 2C07 blocks the activation of PI3K through allosteric Ras modification. 2C07 binds to the modified switch II pocket (S-IIG) of Ras in both GDP- and GTP-bound states, stabilizes the GDP-bound state, disrupts the polar interactions of the canonical GTP-bound state, and inhibits SOS binding and nucleotide exchange. 2C07 can be used in cancer-related research.

EPAC 5376753 (Standard) is the analytical standard of EPAC 5376753 (HY-111446). This product is intended for research and analytical applications. EPAC 5376753, a 2-Thiobarbituric acid (HY-77962) derivative, is a selective and allosteric Epac inhibitor. EPAC 5376753 inhibits Epac1 with an IC₅₀ of 4 µM in Swiss 3T3 cells. EPAC 5376753 does not inhibit PKA and adenylyl cyclases.

GGTI-297 is a geranylgeranyl transferase I (GGTase-1) inhibitor with IC₅₀ values of 56 nM and 203 nM for GGTase-1 and fanesyl transferase (FTase), respectively. GGTI-297 inhibits the processing of the geranylgeranylated protein Rap1A without affecting the farnesylated protein H-Ras.

KRAS G12C inhibitor 62 is a KRAS G12C inhibitor. KRAS G12C inhibitor 62 has the potential for the research of KRAS G12C-mediated cancer (extracted from patent WO2021121367A1).

l-Naproxen (Standard) is the analytical standard of l-Naproxen. This product is intended for research and analytical applications.

Bragsin2 (Standard) is the analytical standard of Bragsin2 (HY-111550). This product is intended for research and analytical applications. Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC₅₀ of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells.

Pipoxolan is an orally active smooth muscle relaxant, anti-inflammatory agent and anticancer agent. Pipoxolan modulates PI3K/AKT signaling pathways, and reduces the levels of Ras/MEK/p-ERK, MMP-2 and MMP-9. Pipoxolan inhibits pro-inflammatory transcription factor pathways, activates Nrf2/HO-1, and suppresses the production of pro-inflammatory mediators. Pipoxolan induces ROS generation, endogenous mitochondrial Apoptosis, and G₀/G₁ cell cycle arrest. Pipoxolan reduces cerebral infarction size and inhibits intimal hyperplasia. Pipoxolan can be used in research related to cerebral ischemia, intimal hyperplasia, oral squamous cell carcinoma, leukemia and lung cancer.

CE3F4 (Standard) is the analytical standard of CE3F4 (HY-108539). This product is intended for research and analytical applications. CE3F4 is a selective antagonist of exchange protein directly activated by cAMP (Epac1), with IC₅₀s of 10.7 μM and 66 μM for Epac1 and Epac2(B), respectively.

CCG-1423 (Standard) is the analytical standard of CCG-1423. This product is intended for research and analytical applications. CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes.

Z52/Z56 intermediate is a key intermediate in the synthesis of RAS inhibitors.

L 731734 is a prodrug of L-731735 (HY-129273), and inhibits Ras processing in cells transformed with v-ras.

Lonafarnib (Standard) (Sch66336 (Standard)) is the analytical standard of Lonafarnib (HY-15136). This product is intended for research and analytical applications. Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria.

XRP44X (Standard) is the analytical standard of XRP44X (HY-107753). This product is intended for research and analytical applications. XRP44X inhibits Ras-induced transcription activation with the IC₅₀ of 10 nM. XRP44X inhibits activation of the Ras-Erk-1/2 pathway by FGF-2. XRP44X is an inhibitor of Ras/Erk activation of Elk3 that also affects microtubules.

Dykellic acid is a RhoA inhibitor. Dykellic acid can inhibit the migration and motility of B16 cells and the tube formation of HUVECs. Dykellic acid is promising for research of cancers.

DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer.

pan-KRAS ligand 1 is a Ligand for Target Protein for PROTAC. pan-KRAS ligand 1 can be used for synthesis PROTAC pan-KRAS degrader 4 (HY-168669).

Daraxonrasib (Standard) is the analytical standard of Daraxonrasib (HY-148439). This product is intended for research and analytical applications. Daraxonrasib (RMC-6236) is an orally active, non-covalent RAS (ON) inhibitor. Daraxonrasib disrupts the interaction of wild-type or mutant RAS proteins with the RAS binding domain of BRAF, with EC₅₀ values ranging from 28-220 nM for wild-type KRAS, NRAS, HRAS, and multiple oncogenic RAS variants. Daraxonrasib inhibits pERK. Daraxonrasib has anti-tumor activity against KRAS mutant tumors.

21-Hydroxyoligomycin A is a potent inhibitor of K-Ras PM localization with an IC₅₀ value of 4.82 nM. 21-Hydroxyoligomycin A has cytotoxicity and can be isolated from Streptomyces.

6-T-GDP (6-Thioguanosine 5'-diphosphate) is a metabolite of azathioprine. 6-T-GDP can reduce the transcription of inflammatory factors and the expression of cell adhesion molecules by inhibiting the activity of Rac1, thereby inhibiting the migration of leukocytes and the occurrence of tissue inflammation.