Trk Receptor|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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TrkA (TRK1-transforming tyrosine kinase protein) is a protein that in humans is encoded by the NTRK1 gene. TrkA is a member of the neurotrophic tyrosine kinase receptor (NTKR) family. TrkA is a membrane-bound receptor that, upon neurotrophin binding, phosphorylates itself (autophosphorylation) and members of the MAPK pathway. TrkA is the high affinity catalytic receptor for the neurotrophin, Nerve Growth Factor, which include neuronal differentiation and avoidance of programmed cell death. The presence of TrkA leads to cell differentiation and may play a role in specifying sensory neuron subtypes. Mutations in TrkA gene have been associated with congenital insensitivity to pain with anhidrosis, self-mutilating behavior, mental retardation and cancer.

TrkB has the highest affinity to the binding of brain-derived neurotrophic factor (BDNF) and NT-4. BDNF is a growth factor that has important roles in the survival and function of neurons in the central nervous system. The binding of BDNF to TrkB receptor causes many intercellular cascades to be activated, which regulate neuronal development and plasticity, long-term potentiation, and apoptosis.

TrkC is ordinarily activated by binding with NT-3 and has little activation by other ligands. (TrkA and TrkB also bind NT-3, but to a lesser extent). TrkC is mostly expressed by proprioceptive sensory neurons.

Cat. No.	Product Name	CAS No.	Information
H8081	TrkA-IN-23	1821484-84-7	TrkA-IN-23 is a highly potent, subtype selective, peripherally restricted, allosteric TrkA inhibitor with IC50 of 10 nM, 180-fold selective over TrkB and 70-fold selective over TrkC in cell based assays; exhibits exquisite TrkA selectivity with >95% inhibition of TrkA and
H8080	Ro 08-2750	37854-59-4	Ro 08-2750 (Ro 082750) is a potent, selective, non-peptide nerve growth factor (NGF) inhibitor that binds to NGF dimer with Kd of 1 uM; selectively inhibits binding of NGF to p75NTR at submicromolar concentrations, and to both p75NTR and TrkA at > 5 uM; inhibits NGF-induced programmed cell death in SK-N-MC cells.
H8079	PQC 083	1563006-38-1	PQC 083 is a novel nerve growth factor (NGF) antagonist with IC50 of 7.0 uM, functionally inhibits NGF's effects on PC12 cell differentiation; PQC 083 is a useful biochemical tool for studying NGF-dependent effects in biochemical or cell biology systems.
H8078	PF-06273340	1402438-74-7	PF-06273340 is a potent and selective, orally bioavailable pan-Trk kinase inhibitor with IC50 of 6, 2, and 1 nM for Trk A, B and C, respectively; displays selectivity over a panel of ion channels, receptors and other enzymes; exhibits in vivo efficacy in a rodent model of inflammatory pain.
H8077	NSC49652	908563-68-8	NSC49652 (NSC 49652) is a compound targeting the transmembrane domain (TMD) of death receptor p75NTR with IC50 of 10 uM in AraTM assays, alters the relative conformation of p75NTR TMDs and induces dynamic changes in the full-length receptor in mammalian cells; induces apoptosis through p75NTR and the JNK pathway in neurons and affects the viability of melanoma cells, reduces tumor growth and improves survival in human melanoma xenograft model, orally available.
H8076	LOXO-195 RS-isomer	2097002-59-8	The RS-isomer of LOXO-195, a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and
H8075	LOXO-195 R racemate	1350884-56-8	The R racemate of LOXO-195, a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and
H8074	LOXO-195	2097002-61-2	LOXO-195 (Selitrectinib,LOXO 195, LOXO195)is a potent, selective, next-generation Trk tyrosine kinase inhibitor with IC50 of 0.6 nM and <2.5 nM for WT TrkA and WT TrKC, respectively; also diplays high potentcy against mutant TrkA G595R, TrkA G667C, TrkC G623R and TrkC G696A with IC50 of 2.0, 9.8, 2.3 and <2.5 nM, respectively; overcomes acquired resistance mediated by recurrent kinase domain (solvent front and xDFG) mutations identified in multiple patients.
H8073	LOXO-101 sulfate	1223405-08-0	LOXO-101 (ARRY-470, Larotrectinib) is potent, selective pan-TRK inhibitor with cellular IC50 of 2-20 nM against TRKA, TRKB, and TRKC kinases; demonstrates excellent selectivity against a panel of 226 non-TRK kinases with one exception (TNK2 IC50=576 nM); inhibits fusion oncoprotein and cellular proliferation in TRK-fusion-bearing human-derived cancer cell lines; markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone; inhibits tumor growth in vivo in TRK fusion-positive cancer models.
H8072	LOXO-101	1223403-58-4	LOXO-101 (ARRY-470, Larotrectinib) is potent, selective pan-TRK inhibitor with cellular IC50 of 2-20 nM against TRKA, TRKB, and TRKC kinases; demonstrates excellent selectivity against a panel of 226 non-TRK kinases with one exception (TNK2 IC50=576 nM); inhibits fusion oncoprotein and cellular proliferation in TRK-fusion-bearing human-derived cancer cell lines; markedly attenuates bone cancer pain and significantly blocks the ectopic sprouting of sensory nerve fibers and the formation of neuroma-like structures in the tumor bearing bone; inhibits tumor growth in vivo in TRK fusion-positive cancer models.

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