Syk (Spleen Tyrosine Kinase)

Sigaling Pathway Map

Research Area

Inhibitory Selectivity

click to view more

Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S2194

R406

R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.

S2206

R788 (Fostamatinib) Disodium

R788 (Fostamatinib) disodium, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.

S1533

R406 (free base)

R406 (free base) is a potent Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.

S8032

PRT062607 (P505-15, BIIB057) HCl

PRT062607 (P505-15, BIIB057) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.

S2625

Fostamatinib (R788)

Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.

S7286New

RO9021

RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.

S7006New

BAY-61-3606

BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM).

S7738New

PRT-060318

PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment.

S3026

Piceatannol

Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.

S4921

MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)

MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.

S7523

Entospletinib (GS-9973)

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay. Phase 2.

Catalog No. Information Product Use Citations Product Validations
S2194

R406

R406 is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.

S2206

R788 (Fostamatinib) Disodium

R788 (Fostamatinib) disodium, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.

S1533

R406 (free base)

R406 (free base) is a potent Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 1.

S8032

PRT062607 (P505-15, BIIB057) HCl

PRT062607 (P505-15, BIIB057) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.

S2625

Fostamatinib (R788)

Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.

S7286New

RO9021

RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.

S7006New

BAY-61-3606

BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM).

S7738New

PRT-060318

PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment.

S3026

Piceatannol

Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.

S4921

MNS (3,4-Methylenedioxy-β-nitrostyrene, MDBN)

MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.

S7523

Entospletinib (GS-9973)

Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay. Phase 2.

Tags: Syk inhibition | Syk signaling | Syk pathway | Syk activation | Syk cancer | Syk phosphorylation | Syk inhibitors in development | Syk signaling pathway | spleen tyrosine kinase pathway | Syk inhibitor review