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Syk Products

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Catalog No. Product Name Information Product Use Citations Product Validations
S0871New Gusacitinib (ASN-002) Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays.
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. R406 (free base) triggers apoptosis. Phase 1.
Theranostics, 2022, 12(5):2232-2247
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
J Virol, 2022, e0020022
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. R406 induces apoptosis. Phase 1.
Theranostics, 2022, 12(5):2232-2247
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
J Virol, 2022, e0020022
S2206 Fostamatinib (R788) disodium Fostamatinib disodium (R788, Tamatinib Fosdium), 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.
Int J Hematol, 2022, 10.1007/s12185-021-03220-9
J Allergy Clin Immunol, 2021, S0091-6749(21)00979-9
Haematologica, 2020, 15;haematol2019241729
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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Int J Hematol, 2022, 10.1007/s12185-021-03220-9
Hum Cell, 2021, 34(6):1911-1918
S3026 Piceatannol Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.
Front Immunol, 2021, 12:766178
Front Vet Sci, 2021, 8:606197
Clin Transl Med, 2021, 11(2):e339
S3226 Dehydroabietic acid Dehydroabietic acid (DAA, DHAA), a naturally occurring diterpene resin acid derived from coniferous plants such as Pinus and Picea, displays anti-inflammatory activity via suppression of Src-, Syk-, and TAK1-mediated pathways.
S3566New Cerdulatinib (PRT062070) Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
S4921 MNS (3,4-Methylenedioxy-β-nitrostyrene) MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.
J Biomol Struct Dyn, 2019, 10.1080/07391102.2019.1640133
Phytomedicine, 2019, 61:152859
Toxicol Res (Camb), 2016, 5(1):188-196
S4944 Fostamatinib disodium hexahydrate Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay.
Int J Hematol, 2022, 10.1007/s12185-021-03220-9
J Allergy Clin Immunol, 2021, S0091-6749(21)00979-9
ScholarsArchive@OSU, 2020, None
S6519 R112 R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM.
S7006 BAY-61-3606 BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis.
JCI Insight, 2021, e149376
Biomed Res, 2021, 42(2):53-66
Nat Cell Biol, 2019, 21(6):778-790
S7286 RO9021 RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.
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 and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.
Cancer Res, 2022, canres.0218.2021
Theranostics, 2022, 12(5):2232-2247
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7634 Cerdulatinib (PRT062070) hydrochloride Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Lett, 2021, 512:28-37
Mol Carcinog, 2021, 60(7):481-496
S7738 PRT-060318 2HCl PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase with an IC50 of 4 nM, as an approach to HIT treatment.
PLoS Pathog, 2022, 18(4):e1010468
FASEB J, 2020, 34(11):15208-15221
Cell Commun Signal, 2019, 17(1):122
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
Mol Cell, 2021, S1097-2765(21)00264-1
Sci Signal, 2021, 14(682)eabc1648
Biochem Pharmacol, 2021, S0006-2952(21)00185-4
S8442 TAK-659 TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
ScholarsArchive@OSU, 2020, 51
ScholarsArchive@OSU, 2020, None
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S9715 Lanraplenib (GS-9876) Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
S0871New Gusacitinib (ASN-002) Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays.
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. R406 (free base) triggers apoptosis. Phase 1.
Theranostics, 2022, 12(5):2232-2247
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
J Virol, 2022, e0020022
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. R406 induces apoptosis. Phase 1.
Theranostics, 2022, 12(5):2232-2247
Free Radic Biol Med, 2022, S0891-5849(22)00004-1
J Virol, 2022, e0020022
S2206 Fostamatinib (R788) disodium Fostamatinib disodium (R788, Tamatinib Fosdium), 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.
Int J Hematol, 2022, 10.1007/s12185-021-03220-9
J Allergy Clin Immunol, 2021, S0091-6749(21)00979-9
Haematologica, 2020, 15;haematol2019241729
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.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Int J Hematol, 2022, 10.1007/s12185-021-03220-9
Hum Cell, 2021, 34(6):1911-1918
S3026 Piceatannol Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.
Front Immunol, 2021, 12:766178
Front Vet Sci, 2021, 8:606197
Clin Transl Med, 2021, 11(2):e339
S3226 Dehydroabietic acid Dehydroabietic acid (DAA, DHAA), a naturally occurring diterpene resin acid derived from coniferous plants such as Pinus and Picea, displays anti-inflammatory activity via suppression of Src-, Syk-, and TAK1-mediated pathways.
S3566New Cerdulatinib (PRT062070) Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
S4921 MNS (3,4-Methylenedioxy-β-nitrostyrene) MNS is a tyrosine kinase inhibitor, inhibits Syk, Src, p97 with IC50 of 2.5 μM, 29.3 μM and 1.7 μM, respectively.
J Biomol Struct Dyn, 2019, 10.1080/07391102.2019.1640133
Phytomedicine, 2019, 61:152859
Toxicol Res (Camb), 2016, 5(1):188-196
S4944 Fostamatinib disodium hexahydrate Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay.
Int J Hematol, 2022, 10.1007/s12185-021-03220-9
J Allergy Clin Immunol, 2021, S0091-6749(21)00979-9
ScholarsArchive@OSU, 2020, None
S6519 R112 R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM.
S7006 BAY-61-3606 BAY-61-3606 is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis.
JCI Insight, 2021, e149376
Biomed Res, 2021, 42(2):53-66
Nat Cell Biol, 2019, 21(6):778-790
S7286 RO9021 RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling.
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 and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.
Cancer Res, 2022, canres.0218.2021
Theranostics, 2022, 12(5):2232-2247
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S7634 Cerdulatinib (PRT062070) hydrochloride Cerdulatinib (PRT-062070, PRT2070) hydrochloride is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Lett, 2021, 512:28-37
Mol Carcinog, 2021, 60(7):481-496
S7738 PRT-060318 2HCl PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase with an IC50 of 4 nM, as an approach to HIT treatment.
PLoS Pathog, 2022, 18(4):e1010468
FASEB J, 2020, 34(11):15208-15221
Cell Commun Signal, 2019, 17(1):122
S8032 PRT062607 (P505-15) HCl PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
Mol Cell, 2021, S1097-2765(21)00264-1
Sci Signal, 2021, 14(682)eabc1648
Biochem Pharmacol, 2021, S0006-2952(21)00185-4
S8442 TAK-659 TAK-659 is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
ScholarsArchive@OSU, 2020, 51
ScholarsArchive@OSU, 2020, None
S8948 SRX3207 SRX3207 is an orally active dual inhibitor of Syk-PI3K with IC50 of 39.9 nM, 31200 nM, 3070 nM, 3070 nM, 244 nM, 388 nM, 9790 nM for Syk, Zap70, BRD41, BRD42, PI3K alpha, PI3K delta, PI3K gamma, respectively. SRX3207 blocks tumor immunosuppression and increases anti-tumor immunity.
S9715 Lanraplenib (GS-9876) Lanraplenib (GS-9876, GS-SYK) is a potent, highly selective and orally active inhibitor of Spleen Tyrosine Kinase (SYK) with IC50 of 9.5 nM. Lanraplenib inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
S0871New Gusacitinib (ASN-002) Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays.
S3566New Cerdulatinib (PRT062070) Cerdulatinib (PRT062070, PRT2070) is an oral active, multi-targeted tyrosine kinase inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. Also inhibits 19 other tested kinases with IC50 less than 200 nM.
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