S2194 |
R406
|
R406(R406 besylate) 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. |
-
Nat Commun, 2024, 15(1):8890
-
J Clin Invest, 2024, e175147
-
J Exp Clin Cancer Res, 2024, 43(1):224
|
|
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. |
-
J Transl Med, 2024, 22(1):283
-
FASEB J, 2024, 38(6):e23564
-
Cancer Res, 2023, 83(2):316-331
|
|
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. |
-
Sci Rep, 2024, 14(1):7739
-
J Exp Med, 2023, 220(9)e20230054
-
J Exp Med, 2023, 220(9)e20230054
|
|
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, 2023, 83(2):316-331
-
Front Immunol, 2023, 14:1279155
-
J Leukoc Biol, 2023, qiad025
|
|
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. |
-
J Thromb Haemost, 2024, S1538-7836(24)00479-3
-
Nat Commun, 2023, 14(1):7576
-
J Exp Med, 2023, 220(9)e20230054
|
|
S3026 |
Piceatannol
|
Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn. |
-
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
-
Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
-
Cell Rep, 2022, 38(13):110567
|
|
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.
|
-
Antimicrob Agents Chemother, 2024, 68(4):e0135023.
-
Int J Mol Sci, 2023, 24(17)13623
-
Cells, 2023, 12(3)453
|
|
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. |
-
FASEB J, 2024, 38(6):e23564
-
Cancer Res, 2023, 83(16):2675-2689
-
Int J Hematol, 2022, 10.1007/s12185-021-03220-9
|
|
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. |
-
Aging (Albany NY), 2024, 16(5):4363-4377
-
Open Life Sci, 2023, 18(1):20220678
-
Nat Commun, 2022, 13(1):6226
|
|
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, 2024, 20(10):e1012674
-
Thromb Haemost, 2024, 10.1055/a-2311-0117
-
Res Pract Thromb Haemost, 2024, 8(7):102582
|
|
S3566 |
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 inhibits19 other tested kinases with IC50 less than 200 nM. |
-
NPJ Precis Oncol, 2024, 8(1):74
-
Int J Mol Sci, 2023, 24(17)13623
-
Cells, 2023, 12(9)1295
|
|
S8442 |
TAK-659 Hydrochloride
|
TAK-659 Hydrochloride 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. |
-
Int J Mol Sci, 2024, 25(18)9914
-
Int J Mol Sci, 2022, 23(23)14706
-
Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
|
|
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. |
-
Phytomedicine, 2019, 61:152859
-
J Biomol Struct Dyn, 2019, 10.1080/07391102.2019.1640133
-
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
|
|
S7286 |
RO9021
|
RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling. |
-
Int J Mol Sci, 2022, 23(23)14706
|
|
S6519 |
R112
|
R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM. |
|
|
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. |
|
|
E1836New |
Cevidoplenib dimesylate
|
Cevidoplenib dimesylate(SKI-O-703 dimesylate) is an orally available inhibitor of spleen tyrosine kinase (Syk) with potential anti-inflammatory and immunomodulating activities. It attenuates the progression of autoantibody-mediated autoimmune diseases by inhibiting both autoantibody-producing and autoantibody-sensing cells. |
|
|
S0871 |
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. |
|
|
S9715 |
Lanraplenib (GS-SYK)
|
Lanraplenib (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. |
-
Cell Rep, 2024, 43(10):114773
|
|
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. |
|
|
E0437 |
ZAP-180013
|
ZAP-180013 is a inhibitor of zeta-chain-associated protein kinase 70 (ZAP-70) with an IC50 of 1.8 μM. |
|
|
E4580New |
Sovleplenib
|
Sovleplenib(HMPL-523) is a highly potent and selective SYK inhibitor with IC50 of 0.025 μM, that exhibits anti-tumor activities in vitro and in vivo. Sovleplenib exhibits synergistic activities in combination with BTK, PI3Kδ, and Bcl2 family inhibitors in killing human-diffused large B cell lymphoma (DLBCL). |
|
|
S2194 |
R406
|
R406(R406 besylate) 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. |
- Nat Commun, 2024, 15(1):8890
- J Clin Invest, 2024, e175147
- J Exp Clin Cancer Res, 2024, 43(1):224
|
|
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. |
- J Transl Med, 2024, 22(1):283
- FASEB J, 2024, 38(6):e23564
- Cancer Res, 2023, 83(2):316-331
|
|
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. |
- Sci Rep, 2024, 14(1):7739
- J Exp Med, 2023, 220(9)e20230054
- J Exp Med, 2023, 220(9)e20230054
|
|
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, 2023, 83(2):316-331
- Front Immunol, 2023, 14:1279155
- J Leukoc Biol, 2023, qiad025
|
|
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. |
- J Thromb Haemost, 2024, S1538-7836(24)00479-3
- Nat Commun, 2023, 14(1):7576
- J Exp Med, 2023, 220(9)e20230054
|
|
S3026 |
Piceatannol
|
Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn. |
- ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
- Sci China Life Sci, 2022, 10.1007/s11427-022-2185-9
- Cell Rep, 2022, 38(13):110567
|
|
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.
|
- Antimicrob Agents Chemother, 2024, 68(4):e0135023.
- Int J Mol Sci, 2023, 24(17)13623
- Cells, 2023, 12(3)453
|
|
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. |
- FASEB J, 2024, 38(6):e23564
- Cancer Res, 2023, 83(16):2675-2689
- Int J Hematol, 2022, 10.1007/s12185-021-03220-9
|
|
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. |
- Aging (Albany NY), 2024, 16(5):4363-4377
- Open Life Sci, 2023, 18(1):20220678
- Nat Commun, 2022, 13(1):6226
|
|
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, 2024, 20(10):e1012674
- Thromb Haemost, 2024, 10.1055/a-2311-0117
- Res Pract Thromb Haemost, 2024, 8(7):102582
|
|
S3566 |
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 inhibits19 other tested kinases with IC50 less than 200 nM. |
- NPJ Precis Oncol, 2024, 8(1):74
- Int J Mol Sci, 2023, 24(17)13623
- Cells, 2023, 12(9)1295
|
|
S8442 |
TAK-659 Hydrochloride
|
TAK-659 Hydrochloride 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. |
- Int J Mol Sci, 2024, 25(18)9914
- Int J Mol Sci, 2022, 23(23)14706
- Am J Physiol Cell Physiol, 2021, 320(5):C902-C915
|
|
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. |
- Phytomedicine, 2019, 61:152859
- J Biomol Struct Dyn, 2019, 10.1080/07391102.2019.1640133
- 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
|
|
S7286 |
RO9021
|
RO9021 potently inhibits SYK kinase activity with an average IC50 of 5.6 nM and suppresses B-cell receptor signaling. |
- Int J Mol Sci, 2022, 23(23)14706
|
|
S6519 |
R112
|
R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM. |
|
|
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. |
|
|
E1836New |
Cevidoplenib dimesylate
|
Cevidoplenib dimesylate(SKI-O-703 dimesylate) is an orally available inhibitor of spleen tyrosine kinase (Syk) with potential anti-inflammatory and immunomodulating activities. It attenuates the progression of autoantibody-mediated autoimmune diseases by inhibiting both autoantibody-producing and autoantibody-sensing cells. |
|
|
S0871 |
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. |
|
|
S9715 |
Lanraplenib (GS-SYK)
|
Lanraplenib (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. |
- Cell Rep, 2024, 43(10):114773
|
|
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. |
|
|
E0437 |
ZAP-180013
|
ZAP-180013 is a inhibitor of zeta-chain-associated protein kinase 70 (ZAP-70) with an IC50 of 1.8 μM. |
|
|
E4580New |
Sovleplenib
|
Sovleplenib(HMPL-523) is a highly potent and selective SYK inhibitor with IC50 of 0.025 μM, that exhibits anti-tumor activities in vitro and in vivo. Sovleplenib exhibits synergistic activities in combination with BTK, PI3Kδ, and Bcl2 family inhibitors in killing human-diffused large B cell lymphoma (DLBCL). |
|
|