Raf

B-Raf IN 16, a BRAF inhibitor, belongs to cyclic iminopyrimidine derivatives and can be used for cancer or tumour research.

B-Raf IN 14 is a BRAF inhibitor.

B-Raf IN 13 is a potent B-Raf inhibitor with anticancer activity.B-Raf IN 13 has an IC50 of 3.55 nM in the BRAF V600E enzyme assay.

B-Raf IN 15 is a BRAF inhibitor that inhibits BRAFWT and BRAFV600E and can be used in the study of melanoma and cancer, and can be optimized for use as a more effective BRA F inhibitor.

Raf inhibitor 2 (CID 25014542) is novel inhibitor of Raf kinases.

B-Raf IN 8 (compound 7g) is a potent inhibitor of B-Raf (IC 50 = 70.65 nM). B-Raf IN 8 shows antitumor activity which has IC 50 values of 9.78, 13.78, 18.52 and 29.85 μM against hepatocellular carcinoma (HEPG-2), colon carcinoma (HCT-116), mammary gland (MCF-7) and human prostate cancer (PC-3) cells [1].

C-RAF kinase-IN-1 is a potent inhibitor of C-RAF kinase with an IC 50 of 0.193 μM. C-RAF kinase-IN-1 is a quinoline derivative. C-RAF kinase-IN-1 has the potential for the research of cancer diseases .

B-Raf inhibitor 1 (B-Raf inhibitor 1) is a potent and selective B-Raf inhibitor.

Raf inhibitor 1 dihydrochloride (B-Raf inhibitor 1 dihydrochloride) is a potent and selective B-Raf inhibitor.

B-Raf IN 6 is a potent inhibitor (IC50: 1.7 nM) of the protein kinase B-Raf, which does not bind the secondary target PXR and is resistant to rapid metabolism.B-Raf IN 6 has shown research potential in cancer diseases.

B-Raf IN 2, compound Ia, is a highly effective and specific inhibitor of BRAF. It exhibits significant potential for cancer research.

PROTAC B-Raf degrader 1 is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf,PROTAC B-Raf degrader 1 With anti-cancer activity.

B-Raf IN 1 is a B-Raf (IC50: 24 nM) and c-Raf (IC50: 25 nM) inhibitor.

Raf inhibitor 3 (Example 30), a potent inhibitor of both B-Raf and C-Raf, exhibits IC50 values below 15 nM. It is applicable in cancer research studies [1].

B-Raf IN 9 (compound 8b) is an effective B-Raf inhibitor (IC50=24.79 nM). B-Raf IN 9 blocks cell cycle at G2/M phase and induces apoptosis. B-Raf IN 9 showed potent anti-tumor activity on human prostate cancer PC-3 cells (IC50=7.83 μM).

RAF mutant-IN-1 is an inhibitor of RAF kinase(IC50 values of 21 nM, 30 nM and 392 nM for C-RAF 340D/Y341D, B-RAFV600E and B-RAFWT, respectively).

RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μμ-15 μμ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity[1]. RAS/RAS-RAF-IN-1 (compound 89; for 4 hours) has an EC50 of 0.5 μμ-5.0 μμ for BRAF-GTP-KRAS-G12C disruption and has an IC50 of 1.0 μμ-10 μμ for pERK inhibition in H358 cells[1]. [1]. Meizhong Jin, et al. Compounds that participate in cooperative binding and uses thereof. WO2020132597A1.

Pan-RAF kinase inhibitor 1 is a potent inhibitor of the Pan-RAF kinase pair that inhibits RAF kinase and regulates MAPK signaling, thereby affecting the proliferation of RAS-mutated tumor cells. Pan-RAF kinase inhibitor 1 has shown research potential for the study of cancer diseases.

B-Raf IN 7 (compound 6a) is a potent inhibitor of B-Raf with an IC 50 of 110.23 nM. B-Raf IN 7 has antitumor activity against colon carcinoma cells(HCT-116), mammary gland cells(MCF-7), hepatocellular carcinoma cells(HEPG-2), human cervical carcinoma cells(Hela) and human prostate cancer cells(PC-3). The IC50 values are 7.50, 9.87, 10.57, 11.63 and 12.83 μM, respectively [1].

RAF-IN-1 is a potent inhibitor of b/cRAF, acting on cRAF (IC50: 3.8 nM), bRAFwt (IC50: 36 nM), bRAFV600E (IC50: 29.4 nM) and inhibiting A375 and H358 cell lines carrying the bRAFV600E mutation with a GI50 of 3.4 and 2.9 nM.

B-Raf IN 5 is a potent inhibitor of the protein kinase B-Raf (IC50: 2.0 nM). B-Raf IN 5 resists rapid metabolism and does not bind to the secondary target PXR.

B-Raf IN 11 is a novel selective inhibitor. The DFG-in conformation of the B-Raf kinase V600E mutant is superior to the DFG-out conformation in colorectal cancer.

RAF709 is a novel Raf kinase inhibitor with IC50s of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.

Uplarafenib (B-Raf IN 10) is a potent BRAF inhibitor with an IC50 in the range of 50-100 nM.B-Raf IN 10 has antitumor activity that may affect cell proliferation and differentiation did not, and can be used to study solid tumors.

Exarafenib (RAF/KIN_2787) is a potent and orally available pan-RAF inhibitor.Exarafenib has antitumor activity and acts by inhibiting downstream MAPK pathway signaling.Exarafenib is used in cancer research.

RAF265 (CHIR-265) (CHIR-265) is a potent selective inhibitor of C-Raf B-Raf B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM. Phase 2.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.

Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.

Belvarafenib is a potent and pan RAF inhibitor with antineoplastic activity. The IC50 values of Belvarafenib are 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively.

Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.

Raffinose (Melitriose) is an indigestible short-chain oligosaccharide, a trisaccharide composed of galactose, glucose and fructose, found in many plants. It can be hydrolyzed by α-galactosidase (α-GAL) to D-galactose and sucrose.

Sarafloxacin (A56620) has antibacterial activities against Gram-positive and Gram-negative bacteria.

1,4-Dipierazino-2,3,5,6-tetrafluorobenzene is a tetrafluorobenzene derivative with a unique structure that allows it to be used as a carrier for drugs, which can be released in a controlled manner, enabling its use in the development of targeted drug delivery systems.

Rafabegron (TAK677) is a potent and selective β3 adrenergic receptor agonist for the study of diabetes and obesity.

BRAF inhibitor is an inhibitor of B-Raf.

Suprafenacine (N'-[(E)-(4-methylphenyl)methylidene]-4,5,6,7-tetrahydro-1H-indazole-3-carbohydrazide) is a cell-permeable microtubule destabilizer that induces cell cycle arrest and apoptosis in G2/M phase. Suprafenacine binds to microtubules and inhibits aggregation at the colchicine junction. Suprafenacine is selective for cancer cells, including drug-resistant cancer cells.

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

Encorafenib (LGX818) is an orally available mutated BRaf V600E inhibitor(IC50=0.3 nM) with potential antineoplastic activity.

Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31/48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.

Sophoraflavanone G (Kushenol F) (Kushenol F), isolated from Sophora flavescens, induces MDA-MB-231 and HL-60 cells apoptosis through suppression of MAPK-related pathways.

AWL-II-38.3 is a highly effective inhibitor of EphA3, a receptor for ephrin-A. It demonstrates potent kinase inhibitory activity against EphA3 and does not show significant cellular activity against Src-family kinases or b-raf [1] [2].

PLX-4720 is a potent and selective inhibitor of B-Raf (V600E) (IC50: 13 nM), equally potent to c-Raf-1(Y340D and Y341D mutations).

LXH254 is a potent C-Raf and B-Raf inhibitor.

Sulindac sulfide (cis-Sulindac sulfide) is a non-steroidal anti-inflammatory compound that has a high affinity for COX-1 and acts as an inhibitor in Ras activation of Raf-1. Sulindac sulfide is a non-competitive inhibitor of gamma-secretase with an IC50 value of 20.2 μM. It is an active metabolite of sulinic acid.

Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes).

Ser-parafluoroPhe-Aad-Leu-Arg-Asn-Pro-NH2 is a biologically active peptide. Structure-activity studies of the thrombin receptor-tethered ligand SFLLRNP underscored the pivotal role of the Phe-2-phenyl group in receptor recognition, while substitution with para-fluorophenylalanine [(p-F)Phe] augmented its activity.

Putraflavone possesses a good antioxidant activity via its DPPH free radical scavenging.

non-selective endothelin receptor agonist

Cudraflavone B has anti-proliferative activity, mouse brain monoamine oxidase (MAO) inhibitory effects, apoptotic actions in human gastric carcinoma cells and mouse melanoma cells, and hepatoprotective activity. It may be a lead for the development of a potential candidate for human oral squamous cell carcinoma cells.

Rafoxanide 13C6 is a labeled Rafoxanide . Rafoxanide is a salicylanilide used as an antiparasitic agent.