Signaling Pathway

Raf

Raf

Related Products

PDF File 0.34MB

Raf kinases are a family of three serine/threonine-specific protein kinases that are related to retroviral oncogenes. RAF is an acronym for Rapidly Accelerated Fibrosarcoma. Raf kinases participate in the RAS-RAF-MEK-ERK signal transduction cascade, also referred to as the mitogen-activated protein kinase (MAPK) cascade. Activation of RAF kinases requires interaction with RAS-GTPases. The three RAF kinase family members are: A-Raf, B-Raf, C-Raf (Raf-1). The B-Raf protein is involved in sending signals inside cells, which are involved in directing cell growth. It was shown to be faulty (mutated) in some human cancers. C-RAF or even Raf-1 is an enzyme that in humans is encoded by the RAF1 gene. The c-Raf protein is part of the ERK1/2 pathway as a MAP kinase kinase kinase (MAP3K) that functions downstream of the Ras subfamily of membrane associated GTPases. C-Raf is a member of the Raf kinase family of serine/threonine-specific protein kinases, from the TKL (Tyrosine-kinase-like) group of kinases.

Raf Inhibitors & Modulators (30)

Product Name Catalog No. Brief Description
AZ 628

HY-11004

AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.

B-Raf IN 1

HY-18227

B-Raf IN 1 is a highlt potent and selective B-Raf inhibitor with IC50 of 24 nM; equipotent against c-Raf (IC50= 25 nM).

B-Raf inhibitor

HY-77251

aA B-Raf inhibitor, pyrazine and pyrrolo[2,3-b]pyridine derivatives, useful in the treatment of cancer and proliferative diseases.

B-Raf inhibitor 1

HY-14177

B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.

B-Raf inhibitor 1 dihydrochloride

HY-14177A

B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.

BRAF inhibitor

HY-10247

BRAF inhibitor is a potent BRAF inhibitor.

CEP-32496

HY-15200

CEP-32496 is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.

CEP-32496 hydrochloride

HY-15199

CEP-32496 Hcl is a highly potent inhibitor of BRAF(V600E/WT) and c-Raf with Kd of 14 nM/36 nM and 39 nM, also potent to Abl-1, c-Kit, Ret, PDGFRβ and VEGFR2, respectively; insignificant affinity for MEK-1, MEK-2, ERK-1 and ERK-2.

Dabrafenib

HY-14660

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.

Dabrafenib Mesylate

HY-14660A

Dabrafenib Mesylate(GSK-2118436 Mesylate) is a novel, potent, and selective Raf kinase inhibitor that is capableof inhibiting the kinase activity of wild-type B-Raf, B-RafV600Eand c-Raf with IC50 values of 3.2, 0.8, and 5.0 nM, respectively.

Doramapimod

HY-10320

Doramapimod (BIRB 796) is a highly selective p38α MAPK inhibitor with Kd of 0.1 nM, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2, ZAP-70, EGFR, HER2, PKA, PKC, PKCα/β/γ.

GDC-0879

HY-50864

GDC-0879 is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM with activity against c-Raf as well; no inhibition known to other protein kinases.

GW 5074

HY-10542

GW 5074 is a potent, selective and cell-permeable c-Raf1 kinase inhibitor (IC50 = 9 nM); displays ≥ 100-fold selectivity for raf kinase over CDK1, CDK2, c-src, ERK2, MEK, p38, Tie2, VEGFR2 and c-fms.

HG6-64-1

HY-12291

HG6-64-1 is a potent and selective B-Raf  and mutant B-Raf inhibitor; more information can be found in Patent WO 2011090738.

L-779450

HY-12787

L-779450 is a potent, ATP-competitive Raf kinase inhibitor (IC50 =10 nM) that displays > 7, > 30 and > 70-fold selectivity over p38α, GSK3β and Lck respectively.

LGX818

HY-15605

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

LY3009120

HY-12558

LY3009120 is a small molecule that has been shown in vitro to be a pan-RAF inhibitor of all isoforms, blocking proliferation in both BRAF and RAS mutant cells.

MLN 2480

HY-15246

MLN 2480(BIIB-024) is an oral, selective pan-Raf kinase inhibitor in chinical trials.

PLX-4720

HY-51424

PLX 4720 is a potent and selective inhibitor of B-RafV600E(IC50=13 nM) and c-Raf-1Y340D/Y341D(IC50=6.7 nM); 10-fold selectivity for B-RafV600E than wild-type B-Raf.

PLX7904

HY-18997

PLX7904 is a Raf inhibitor, inhibits the growth of two melanoma cell lines (A375 and COLO829) and human colorectal cancer cell line COLO205 that expressed BRAFV600E with IC50 values of 0.17 μM, 0.53 μM, and 0.16 μM, respectively.