Raf Inhibitor

B-Raf IN 6 (compound 2c) is a potent inhibitor of protein kinase B-Raf with an IC₅₀ of 1.7 nM. B-Raf IN 6 is devoid of binding to the secondary target PXR and resists rapid metabolism. B-Raf IN 6 has the potential for the research of cancer disease.

SB-590885 GMP is SB-590885 (HY-10966) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. SB-590885 is a BRAF/c-Raf kinase inhibitor that selectively targets B-Raf, and it amplifies the ERK/MAPK signaling pathway in RAS-activated cells. SB-590885 effectively inhibits the malignant proliferation, transformation and tumorigenicity of oncogenic B-Raf cells; it also induces the proliferation of erythroid progenitor cells, delays their differentiation and promotes hemoglobin synthesis, thereby improving ineffective erythropoiesis and reducing apoptosis. SB-590885 exerts a synergistic effect with TGF-β inhibitors and glucocorticoids, significantly promoting the formation of erythroid colonies in cells from patients with Diamond-Blackfan anemia (DBA). SB-590885 is mainly used in relevant studies on DBA, cisplatin-induced myelosuppression-related anemia, and pan-cancers such as melanoma and colorectal cancer.

KRAS-IN-55 is a pan-KRAS inhibitor with IC₅₀ values of 4.3, 9.6 and 1.6 nM against KRAS^G12C, KRAS^G12D and KRAS^G12V, respectively. KRAS-IN-55 induces the formation of a new binding pocket on KRAS, thereby forming a high-affinity ternary complex with cyclophilin A (CYPA), inhibiting the interactions of KRAS with downstream effectors RAF and PI3K, and blocking oncogenic MAPK and PI3K signaling pathways. KRAS-IN-55 is applicable to cancer research such as colorectal cancer and non-small cell lung cancer.

MEK-IN-10 is an orally active pan-MEK/RAF non-degrading molecular glue with an IC₅₀ of 782 nM against human MEK1. MEK-IN-10 blocks the phosphorylation of MEK and ERK, induces and stabilizes the MEK1-RAF complex, and disrupts the RAS-MAPK signaling pathway. MEK-IN-10 induces apoptosis in cancer cells and arrests cells at the G0/G1 phase. MEK-IN-10 induces tumor growth inhibition in mouse xenograft models. MEK-IN-10 can be used in the research of RAS-driven cancers, such as colorectal cancer and pancreatic cancer.

BRAF V600E/CRAF-IN-1 (Compound 8b) is a potent inhibitor of BRAF ^V600E/CRAF. BRAF V600E/CRAF-IN-1 triggers apoptosis and cell cycle arrest at G0/G1 phase in HCT-116 colon cancer cell. BRAF V600E/CRAF-IN-1 has the potential for the research of cancer diseases.

Erufosine is an inhibitor of PI3K/Akt and Ras/Raf/MAPK signaling pathways. Erufosine inhibits the activity of breast cancer cell lines MCF-7 and MDA-MB 231 (IC₅₀: 40.95/40.8 μM). Erufosine reduces the phosphorylation of PI3K (p85), Akt (PKB), and cRaf. Erufosine can be used in the study of breast cancer and myeloid leukemia.

COX/5-LO-IN-2 is a COX2, EGFR, COX1, 5-LOX, BRAF and FAK inhibitor with IC₅₀ of 1.22 μM, 2.5 μM, 2.95 μM, 4.65 μM, 7.4 μM, 12.2 μM, respectively. COX/5-LO-IN-2 induces cell growth arrest at G2/M phase. COX/5-LO-IN-2 triggers apoptotic activity by up-regulating proapoptotic proteins p53, Bax, and caspase-7 and down-regulating anti-apoptotic protein Bcl-2. COX/5-LO-IN-2 can be used for the research of breast cancer.

EGFR/BRAFV600E-IN-6 (Compound 7c) is a dual EGFR/BRAF^V600E inhibitor with IC₅₀ values of 0.12 and 0.05 μM. EGFR/BRAFV600E-IN-6 can activate caspase-3/8/9, unregulate Bax expression and downregulate Bcl-2 levels. EGFR/BRAFV600E-IN-6 can induce apoptosis and shows antioxidant activity. EGFR/BRAFV600E-IN-6 can be used for the research of cancer, such as colon cancer.

EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAF^V600E dual inhibitor with IC₅₀s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC₅₀s of 1.2, 0.79, 1.3, and 1.23 µM, respectively.

RAF-IN-1 is a RAF inhibitor with IC₅₀ values ​​of 29.4 nM, 3.8 nM, and 36 nM against human recombinant bRAF^V600E, cRAF, and bRAF^WT enzymes, respectively. RAF-IN-1 suppresses RAF enzymatic activity and reduces cancer cell proliferation. RAF-IN-1 can be used for cancer research.

Multi-target kinase-IN-8 (3d) is an anti-cancer agent. Multi-target kinase-IN-8 exhibits inhibitory activity against various protein kinases (B-Raf V600E (IC₅₀ = 0.078 µg/mL), c-Met (IC₅₀ = 0.405 µg/mL), Pim-1 (IC₅₀ = 1.053 µg/mL), EGFR WT (IC₅₀ = 0.177 µg/mL), VEGFR-2 (IC₅₀ = 0.275 µg/mL)). Multi-target kinase-IN-8 can induce cell cycle arrest and promote early and late apoptosis. Multi-target kinase-IN-8 is commonly used in cancer research.

CCT239065 is an orally available, effective inhibitor of the mutant protein kinase ^V600EBRAF (RAF) with anti-tumor activity. CCT239065 inhibits downstream signaling of ^V600EBRAF in cancer cells, blocking DNA synthesis and suppressing proliferation.

B-Raf IN 14 (Comp 25) is a BRAF inhibitor with IC₅₀ value of 11.08 μM, which can be used in cancer-related research.

MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer.

VEGFR2/C-RAF kinase-IN-1 is a type II dual kinase inhibitor targeting VEGFR2 and C-RAF, with IC₅₀ values of 12.22 nM and 38.04 nM, respectively. VEGFR2/C-RAF kinase-IN-1 binds VEGFR2 and CRAF in a Type-II mode and inhibits the downstream Raf-MEK-ERK signaling cascade. VEGFR2/C-RAF kinase-IN-1 induces cell cycle arrest, apoptosis, and intracellular ROS accumulation in H1299 cells, while partially inhibiting P-gp efflux function. VEGFR2/C-RAF kinase-IN-1 can be used for cancer research, such as non-small cell lung cancer and liver cancer.

ISIS 5132 sodium scrambled negative control is the sequence scrambled negative control of ISIS 5132 sodium.

NEPP11 is a cyclopentenone prostaglandin analogue. NEPP11 can inhibit glutamate-induced HT22 cell death in mouse hippocampus and prevent manganese-induced apoptosis in PC12 cells. NEPP11 can activate Nrf2 and maintain MEK1/2 and ERK1/2 activity by inhibiting c-Raf downregulation. NEPP11 exerts a neuroprotective effect in a mouse model of focal cerebral ischemia caused by permanent middle cerebral artery occlusion.

AD57 hydrochloride is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src.

KRAS-IN-58 is a KRAS inhibitor with a IC₅₀ of 0.223 μM against KRAS^G12D. KRAS-IN-58 binds to KRAS^G12C and KRAS^G12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer.

Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC₅₀ of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC₅₀ of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats.