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Catalog No. Product Name Information Product Use Citations Product Validations
S0020 RK 24466 RK-24466 (KIN 001-51, Lck inhibitor C 8863, C8863) is a potent and selective inhibitor of Lck that inhibits two constructs of the human lck kinase, lck (64-509) and lckcd with IC50 of < 0.001 μM and 0.002 μM, respectively.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
S0791 eCF506 eCF506 is a potent, selective and orally bioavailable inhibitor of Src tyrosine kinase with IC50 < 0.5 nM.
Oncogene, 2021, 10.1038/s41388-021-02029-4
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Front Pharmacol, 2022, 13:807440
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00383-4
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
J Immunother Cancer, 2022, 10(1)e003766
Front Oncol, 2022, 12:802482
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
Cancer Cell, 2022, S1535-6108(21)00662-0
J Immunother Cancer, 2022, 10(1)e003766
NPJ Precis Oncol, 2022, 6(1):16
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
S1392 Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1490 Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
J Immunother Cancer, 2022, 10(1)e003766
JCI Insight, 2022, 7(7)e154824
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S1574 Doramapimod (BIRB 796) Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.
Biology (Basel), 2022, 11(1)121
Immunity, 2021, S1074-7613(21)00403-9
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
S2202 NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
Cell Rep, 2021, 35(1):108940
Mol Ther Nucleic Acids, 2021, 25:328-341
Cancer Lett, 2020, 475:53-64
S2213 AMG-47a AMG-47a is a potent, nonselective inhibitor of Lck kinase with IC50 of 3.4 uM and it also inhibits T cell proliferation. AMG-47a exhibit anti-inflammatory activity (ED50) of 11 mg/kg in the anti-CD3-induced production of interleukin-2 (IL-2) in mice.
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
Nucleic Acids Res, 2021, gkab538
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S2700 KX2-391 (Tirbanibulin) KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
Signal Transduct Target Ther, 2022, 7(1):35
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cell Rep, 2022, 38(12):110548
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.
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
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Front Oncol, 2021, 11:739139
Biochem Biophys Res Commun, 2021, 586:177-184
Cells, 2020, 9(6):E1452
S5254 Dasatinib hydrochloride Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
NPJ Precis Oncol, 2022, 6(1):16
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
S5548 7-Hydroxy-4-chromone 7-Hydroxychromone is an inhibitor of Src kinase with IC50 of <300 μM.
S5617 Myristic Acid Myristic acid (Tetradecanoic acid) is a fatty acid that occurs naturally in some foods. Myristic acid inhibits the phosphorylation of poly E4Y by Src with an Ki of 35 μM.
S6060 HPK1-IN-2 HPK1-IN-2 is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1, a serine/threonine Ste20-related protein kinase), Lck and Flt3 with IC50 of <0.05 μM, IC50 of <0.5 μM and IC50 of <0.05 μM, respectively. HPK1-IN-2 exhibits antitumor activity.
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S6500 KX1-004 KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).
S6567 Src Inhibitor 1 Src Inhibitor 1 is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.
PLoS Biol, 2022, 20(1):e3001518
S7008 PP2 PP2 (AG 1879, AGL 1879), a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
Cancer Commun (Lond), 2022, 42(3):205-222
Environ Toxicol, 2022, 10.1002/tox.23469
Nat Cell Biol, 2021, 23(1):75-86
S7060 PP1 PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Front Immunol, 2021, 12:737988
Cell Rep, 2020, 30(6):1780-1797
S7565 WH-4-023 WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
Cell Res, 2021, 10.1038/s41422-021-00592-9
Proc Natl Acad Sci U S A, 2021, 118(15)e2018505118
Front Cell Dev Biol, 2021, 9:785055
S7743 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Cell Rep, 2019, 29(3):573-588
S7774 SU6656 SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
Nat Commun, 2021, 12(1):2699
Neuro Oncol, 2021, noab158
Front Immunol, 2021, 12:737988
S7782 Dasatinib Monohydrate Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
NPJ Precis Oncol, 2022, 6(1):16
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
Front Oncol, 2022, 12:802482
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
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S8518 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.
Mol Cancer Res, 2020, 1176-1188
Mol Cancer Res, 2020, 18(8):1176-1188
Mol Cancer Res, 2020, 27;molcanres.1245.2019
S8583 Repotrectinib (TPX-0005) Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
Cancer Res, 2022, canres.1397.2021
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2020, clincanres.2585.2020
S8706 UM-164 UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
S9620New Elzovantinib (TPX-0022) Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.
S9643 DGY-06-116 DGY-06-116 is an irreversible covalent and selective inhibitor of Src with IC50 of 2.6 nM.
S9826New TPX-0046

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.

A5066 Src Rabbit Recombinant mAb Src Rabbit Recombinant mAb detects endogenous levels of total Src.
Cell Rep, 2019, 29(5):1311-1322.e5
S8321 MLR-1023 MLR-1023 (Tolimidone, CP-26154) is a Lyn kinase activator and a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes.
S0020 RK 24466 RK-24466 (KIN 001-51, Lck inhibitor C 8863, C8863) is a potent and selective inhibitor of Lck that inhibits two constructs of the human lck kinase, lck (64-509) and lckcd with IC50 of < 0.001 μM and 0.002 μM, respectively.
Cell Chem Biol, 2021, S2451-9456(21)00303-2
S0791 eCF506 eCF506 is a potent, selective and orally bioavailable inhibitor of Src tyrosine kinase with IC50 < 0.5 nM.
Oncogene, 2021, 10.1038/s41388-021-02029-4
S0918 Ginkgolic acid C17:1 Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3.
Front Pharmacol, 2022, 13:807440
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Cancer Cell, 2021, S1535-6108(21)00383-4
S1014 Bosutinib (SKI-606) Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy.
J Immunother Cancer, 2022, 10(1)e003766
Front Oncol, 2022, 12:802482
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S1021 Dasatinib (BMS-354825) Dasatinib (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity.
Cancer Cell, 2022, S1535-6108(21)00662-0
J Immunother Cancer, 2022, 10(1)e003766
NPJ Precis Oncol, 2022, 6(1):16
S1181 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.
Cell, 2021, 184(2):334-351.e20
Sci Adv, 2021, 7(4)eabd7851
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
S1272 XL228 XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively.
S1392 Pelitinib (EKB-569) Pelitinib (EKB-569) is a potent irreversible EGFR inhibitor with IC50 of 38.5 nM. Pelitinib (EKB-569) also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282 nM, 800 nM and 1255 nM, respectively. Phase2.
Sci Rep, 2022, 12(1):2928
Mol Cancer Ther, 2020, 5;molcanther.1131.2019
Nat Cell Biol, 2019, 21(6):778-790
S1396 Resveratrol (SRT501) Resveratrol (SRT501, trans-Resveratrol) has a wide spectrum of targets including cyclooxygenases(i.e. COX, IC50=1.1 μM), lipooxygenases(LOX, IC50=2.7 μM), kinases, sirtuins and other proteins. It has anti-cancer, anti-inflammatory, blood-sugar-lowering and other beneficial cardiovascular effects. Resveratrol induces mitophagy/autophagy and autophagy-dependent apoptosis.
Int Immunopharmacol, 2022, 103:108489
Eur J Neurosci, 2022, 10.1111/ejn.15596
Adv Sci (Weinh), 2021, e2103360
S1490 Ponatinib (AP24534) Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.
J Immunother Cancer, 2022, 10(1)e003766
JCI Insight, 2022, 7(7)e154824
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
S1574 Doramapimod (BIRB 796) Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with Kd of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.
Biology (Basel), 2022, 11(1)121
Immunity, 2021, S1074-7613(21)00403-9
Proc Natl Acad Sci U S A, 2021, 118(38)e2102423118
S2202 NVP-BHG712 NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
Cell Rep, 2021, 35(1):108940
Mol Ther Nucleic Acids, 2021, 25:328-341
Cancer Lett, 2020, 475:53-64
S2213 AMG-47a AMG-47a is a potent, nonselective inhibitor of Lck kinase with IC50 of 3.4 uM and it also inhibits T cell proliferation. AMG-47a exhibit anti-inflammatory activity (ED50) of 11 mg/kg in the anti-CD3-induced production of interleukin-2 (IL-2) in mice.
S2391 Quercetin (NSC 9221) Quercetin (NSC 9221, Sophoretin, C.I. 75720), a natural flavonoid present in vegetables, fruit and wine, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4-5.4 μM. Quercetin induces mitophagy, apoptosis and protective autophagy. Phase 4.
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Mol Neurobiol, 2022, 10.1007/s12035-021-02712-3
Nucleic Acids Res, 2021, gkab538
S2622 PP121 PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.
Life Sci Alliance, 2021, 4(2)e202000882
PLoS One, 2016, 11(10):e0164895
Biochem Biophys Res Commun, 2015, 465(1):137-44
S2642 1-Naphthyl PP1(1-NA-PP1) 1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively.
S2700 KX2-391 (Tirbanibulin) KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
Signal Transduct Target Ther, 2022, 7(1):35
Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7
Cell Rep, 2022, 38(12):110548
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.
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
S5248 Apatinib Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis.
Front Oncol, 2021, 11:739139
Biochem Biophys Res Commun, 2021, 586:177-184
Cells, 2020, 9(6):E1452
S5254 Dasatinib hydrochloride Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
NPJ Precis Oncol, 2022, 6(1):16
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
S5548 7-Hydroxy-4-chromone 7-Hydroxychromone is an inhibitor of Src kinase with IC50 of <300 μM.
S5617 Myristic Acid Myristic acid (Tetradecanoic acid) is a fatty acid that occurs naturally in some foods. Myristic acid inhibits the phosphorylation of poly E4Y by Src with an Ki of 35 μM.
S6060 HPK1-IN-2 HPK1-IN-2 is a potent and orally active inhibitor of hematopoietic progenitor kinase-1 (HPK1, a serine/threonine Ste20-related protein kinase), Lck and Flt3 with IC50 of <0.05 μM, IC50 of <0.5 μM and IC50 of <0.05 μM, respectively. HPK1-IN-2 exhibits antitumor activity.
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S6500 KX1-004 KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM).
S6567 Src Inhibitor 1 Src Inhibitor 1 is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.
PLoS Biol, 2022, 20(1):e3001518
S7008 PP2 PP2 (AG 1879, AGL 1879), a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
Cancer Commun (Lond), 2022, 42(3):205-222
Environ Toxicol, 2022, 10.1002/tox.23469
Nat Cell Biol, 2021, 23(1):75-86
S7060 PP1 PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
Nat Chem Biol, 2021, 10.1038/s41589-021-00772-z
Front Immunol, 2021, 12:737988
Cell Rep, 2020, 30(6):1780-1797
S7565 WH-4-023 WH-4-023 (KIN001-112, KIN112, Dual LCK/SRC inhibitor) is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
Cell Res, 2021, 10.1038/s41422-021-00592-9
Proc Natl Acad Sci U S A, 2021, 118(15)e2018505118
Front Cell Dev Biol, 2021, 9:785055
S7743 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
Cell Rep, 2019, 29(3):573-588
S7774 SU6656 SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
Nat Commun, 2021, 12(1):2699
Neuro Oncol, 2021, noab158
Front Immunol, 2021, 12:737988
S7782 Dasatinib Monohydrate Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
NPJ Precis Oncol, 2022, 6(1):16
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
Front Oncol, 2022, 12:802482
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
S8161 ON123300 ON123300 is a potent and multi-targeted kinase inhibitor with IC50 of 3.9 nM, 5 nM, 26 nM, 26 nM, 9.2 nM and 11nM for CDK4, Ark5/NUAK1, PDGFRβ, FGFR1, RET (c-RET), and Fyn, respectively.
J Cell Sci, 2021, jcs.258685
Molecules, 2020, 8;25(9) pii: E2220
S8518 AD80 AD80, a multikinase inhibitor, shows strong activity against human RET (c-RET), BRAF, S6K, and SRC but were much less active than either AD57 or AD58 against mTOR. The IC50 value for RET is 4 nM.
Mol Cancer Res, 2020, 1176-1188
Mol Cancer Res, 2020, 18(8):1176-1188
Mol Cancer Res, 2020, 27;molcanres.1245.2019
S8583 Repotrectinib (TPX-0005) Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); also a potent SRC inhibitor (IC50 5.3 nM).
Cancer Res, 2022, canres.1397.2021
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2020, clincanres.2585.2020
S8706 UM-164 UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.
S9620New Elzovantinib (TPX-0022) Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.
S9643 DGY-06-116 DGY-06-116 is an irreversible covalent and selective inhibitor of Src with IC50 of 2.6 nM.
S9826New TPX-0046

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.

A5066 Src Rabbit Recombinant mAb Src Rabbit Recombinant mAb detects endogenous levels of total Src.
Cell Rep, 2019, 29(5):1311-1322.e5
S8321 MLR-1023 MLR-1023 (Tolimidone, CP-26154) is a Lyn kinase activator and a novel insulin receptor potentiator that elicits a rapid-onset and durable improvement in glucose homeostasis in animal models of type 2 diabetes.
S6383New 1-NM-PP1 1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively.
S9620New Elzovantinib (TPX-0022) Elzovantinib (TPX-0022, CSF1R-IN-2) is a potent inhibitor of MET/CSF1R/SRC with enzymatic kinase inhibition IC50s of 0.14 nM, 0.71 nM and 0.12 nM, respectively. TPX-0022 modulates the tumor immune microenvironment in preclinical models.
S9826New TPX-0046

TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay.

Tags: Src activation | Src kinase family | Src family kinases | Src activity | Src cancer | Src tyrosine kinase | Src pathway | Src phosphorylation | Src inhibition | Src kinase pathway | Src kinase assay | Src inhibitors cancer | Src inhibitor clinical trials | Src inhibitor review