Signaling Pathway

Raf

Raf

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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 (31)

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.

CCT196969

HY-12846

CCT196969, a pan-Raf inhibitor, inhibits B-Raf with an IC50 of 0.1 μM.

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.