S1021 |
Dasatinib
|
Dasatinibは新規の強力なマルチターゲット阻害剤であり、cell-free assy における Abl, Src および c-Kit に対する IC50 はそれぞれ < 1 nM, 0.8 nM および 79 nM です。Dsatinib はオートファジー (autophagy) とアポトーシス (apoptosis) を誘発し、抗腫瘍活性を示します。 |
-
Nature, 2024, 10.1038/s41586-024-07079-8
-
Cell Rep Med, 2024, 5(2):101416
-
Cell Rep Med, 2024, 5(2):101412
|
|
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. |
-
Nat Commun, 2024, 15(1):1300
-
Nat Cancer, 2023, 4(2):240-256
-
Cancer Res, 2023, 83(1):141-157
|
|
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.
|
-
bioRxiv, 2023, 2023.05.11.540170
-
Nat Cell Biol, 2022, 24(7):1049-1063
-
J Biomed Sci, 2022, 29(1):42
|
|
S1490 |
Ponatinib
|
Ponatinib 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. |
-
Mol Cancer, 2023, 10.1186/s12943-023-01837-4
-
Clin Cancer Res, 2023, 29(16):3151-3161
-
Cell Death Dis, 2023, 14(7):463
|
|
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. |
-
Commun Biol, 2023, 6(1):872
-
Commun Biol, 2023, 6(1):872
-
Commun Biol, 2023, 6(1):872
|
|
S1010 |
Nintedanib
|
Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3. |
-
Invest Ophthalmol Vis Sci, 2024, 65(2):30
-
Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
-
Elife, 2023, 12e79840
|
|
S1014 |
Bosutinib
|
Bosutinib 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. |
-
Heliyon, 2024, 10(1):e23690
-
Mol Cell, 2023, 83(5):803-818.e8
-
Cancer Res, 2023, 83(1):141-157
|
|
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. |
-
Aging Cell, 2024, e14093.
-
Cell Rep, 2023, 42(6):112547
-
Int J Mol Sci, 2023, 10.3390/ijms242216538
|
|
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. |
-
J Pain, 2023, S1526-5900(23)00013-5
-
J Ovarian Res, 2023, 16(1):122
-
Mol Med Rep, 2023, 28(3)161
|
|
S1396 |
Resveratrol
|
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. |
-
J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
-
Cell Death Dis, 2023, 14(6):367
-
Antiviral Res, 2023, 216:105674
|
|
S8032 |
PRT062607 (P505-15) HCl
|
PRT062607 (P505-15, BIIB057, PRT-2607) 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. |
-
J Exp Med, 2023, 220(9)e20230054
-
Adv Sci (Weinh), 2023, 10(10):e2205397
-
J Thromb Haemost, 2023, 21(8):2236-2247
|
|
S2391 |
Quercetin
|
Quercetin, 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. |
-
MedComm (2020), 2023, 4(5):e346
-
MedComm -2020), 2023, 4(5):e346
-
Aging Cell, 2023, e13771.
|
|
S2700 |
Tirbanibulin
|
Tirbanibulin, 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. |
-
Adv Sci (Weinh), 2023, 10(7):e2202956
-
Cancers (Basel), 2023, 15(7)2189
-
Signal Transduct Target Ther, 2022, 7(1):35
|
|
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.
|
-
Cell Rep Med, 2023, S2666-3791(23)00002-2
-
Autophagy, 2023, 1-20.
-
Cell Rep, 2023, 42(4):112324
|
|
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 Commun, 2023, 14(1):4269
-
Nat Commun, 2023, 186(22):4851-4867.e20
-
J Transl Med, 2023, 21(1):89
|
|
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. |
-
Sci Rep, 2024, 14(1):879
-
Adv Sci (Weinh), 2023, 10(23):e2300898
-
J Thorac Oncol, 2023, S1556-0864(23)00802-X
|
|
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.
|
-
Nat Commun, 2024, 15(1):668
-
Cell Stem Cell, 2023, 30(9):1235-1245.e6
-
Protein Cell, 2023, 14(5):337-349
|
|
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, 2022, 41(11):111827
-
Oncogene, 2022, 10.1038/s41388-022-02519-z
-
Cell Rep, 2021, 35(1):108940
|
|
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 Discov, 2023, 13(3):598-615
-
EMBO Mol Med, 2023, 10.15252/emmm.202217367
-
Cancer Res, 2022, canres.1397.2021
|
|
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. |
-
Cancer Cell, 2022, S1535-6108(22)00312-9
-
Cancer Discov, 2022, 12(5):1378-1395
-
Cell Oncol (Dordr), 2022, 45(4):601-619
|
|
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
|
|
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. |
-
Nat Commun, 2022, 13(1):2500
-
Mol Cancer Res, 2020, 18(8):1176-1188
-
Mol Cancer Res, 2020, 1176-1188
|
|
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
-
PLoS One, 2016, 11(10):e0164895
|
|
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
|
|
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. |
-
Sci Adv, 2024, 10(6):eadi4935
-
PLoS Biol, 2022, 20(1):e3001518
-
Front Cell Dev Biol, 2022, 10:942718
|
|
S7743 |
CCT196969
|
CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
-
Nat Commun, 2022, 13(1):7113
-
Cell Rep, 2019, 29(3):573-588
|
|
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
|
|
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
|
|
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. |
-
Nat Commun, 2023, 14(1):660
|
|
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
|
|
S8321 |
Tolimidone (MLR-1023)
|
Tolimidone (MLR-1023) is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals. |
-
Biochemical Pharmacology, 2023, Volume 211
|
|
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. |
-
Cancers (Basel, 2022, 14(215343)
|
|
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. |
|
|
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. |
|
|
S6500 |
KX1-004
|
KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM). |
|
|
S5548 |
7-Hydroxy-4-chromone
|
7-Hydroxychromone is an inhibitor of Src kinase with IC50 of <300 μM. |
|
|
S9643 |
DGY-06-116
|
DGY-06-116 is an irreversible covalent and selective inhibitor of Src with IC50 of 2.6 nM. |
|
|
S9620 |
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. |
|
|
E0814 |
Masitinib mesylate
|
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK. |
|
|
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. |
|
|
E2202 |
1-Naphthyl PP1 hydrochloride
|
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively. |
|
|
E2643 |
TL02-59
|
TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. |
|
|
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. |
|
|
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. |
|
|
S9826 |
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. |
|
|
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. |
|
|
S6383 |
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. |
|
|
E1634New |
CH6953755
|
CH6953755 is a potent, orally active, and selective inhibitor of YES1 kinase with an IC50 of 1.8 nM. CH6953755 demonstrates antitumor activity against YES1 gene-amplified cancers. |
|
|
S1021 |
Dasatinib
|
Dasatinibは新規の強力なマルチターゲット阻害剤であり、cell-free assy における Abl, Src および c-Kit に対する IC50 はそれぞれ < 1 nM, 0.8 nM および 79 nM です。Dsatinib はオートファジー (autophagy) とアポトーシス (apoptosis) を誘発し、抗腫瘍活性を示します。 |
- Nature, 2024, 10.1038/s41586-024-07079-8
- Cell Rep Med, 2024, 5(2):101416
- Cell Rep Med, 2024, 5(2):101412
|
|
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. |
- Nat Commun, 2024, 15(1):1300
- Nat Cancer, 2023, 4(2):240-256
- Cancer Res, 2023, 83(1):141-157
|
|
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.
|
- bioRxiv, 2023, 2023.05.11.540170
- Nat Cell Biol, 2022, 24(7):1049-1063
- J Biomed Sci, 2022, 29(1):42
|
|
S1490 |
Ponatinib
|
Ponatinib 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. |
- Mol Cancer, 2023, 10.1186/s12943-023-01837-4
- Clin Cancer Res, 2023, 29(16):3151-3161
- Cell Death Dis, 2023, 14(7):463
|
|
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. |
- Commun Biol, 2023, 6(1):872
- Commun Biol, 2023, 6(1):872
- Commun Biol, 2023, 6(1):872
|
|
S1010 |
Nintedanib
|
Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3. |
- Invest Ophthalmol Vis Sci, 2024, 65(2):30
- Cell Death Dis, 2023, 10.1038/s41419-023-06240-x
- Elife, 2023, 12e79840
|
|
S1014 |
Bosutinib
|
Bosutinib 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. |
- Heliyon, 2024, 10(1):e23690
- Mol Cell, 2023, 83(5):803-818.e8
- Cancer Res, 2023, 83(1):141-157
|
|
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. |
- Aging Cell, 2024, e14093.
- Cell Rep, 2023, 42(6):112547
- Int J Mol Sci, 2023, 10.3390/ijms242216538
|
|
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. |
- J Pain, 2023, S1526-5900(23)00013-5
- J Ovarian Res, 2023, 16(1):122
- Mol Med Rep, 2023, 28(3)161
|
|
S1396 |
Resveratrol
|
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. |
- J Hazard Mater, 2023, 10.1016/j.jhazmat.2023.132932
- Cell Death Dis, 2023, 14(6):367
- Antiviral Res, 2023, 216:105674
|
|
S8032 |
PRT062607 (P505-15) HCl
|
PRT062607 (P505-15, BIIB057, PRT-2607) 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. |
- J Exp Med, 2023, 220(9)e20230054
- Adv Sci (Weinh), 2023, 10(10):e2205397
- J Thromb Haemost, 2023, 21(8):2236-2247
|
|
S2391 |
Quercetin
|
Quercetin, 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. |
- MedComm (2020), 2023, 4(5):e346
- MedComm -2020), 2023, 4(5):e346
- Aging Cell, 2023, e13771.
|
|
S2700 |
Tirbanibulin
|
Tirbanibulin, 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. |
- Adv Sci (Weinh), 2023, 10(7):e2202956
- Cancers (Basel), 2023, 15(7)2189
- Signal Transduct Target Ther, 2022, 7(1):35
|
|
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.
|
- Cell Rep Med, 2023, S2666-3791(23)00002-2
- Autophagy, 2023, 1-20.
- Cell Rep, 2023, 42(4):112324
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S7060 |
PP1
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PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM. |
- Nat Commun, 2023, 14(1):4269
- Nat Commun, 2023, 186(22):4851-4867.e20
- J Transl Med, 2023, 21(1):89
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S5248 |
Apatinib
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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. |
- Sci Rep, 2024, 14(1):879
- Adv Sci (Weinh), 2023, 10(23):e2300898
- J Thorac Oncol, 2023, S1556-0864(23)00802-X
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S7565 |
WH-4-023
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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.
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- Nat Commun, 2024, 15(1):668
- Cell Stem Cell, 2023, 30(9):1235-1245.e6
- Protein Cell, 2023, 14(5):337-349
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S2202 |
NVP-BHG712
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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, 2022, 41(11):111827
- Oncogene, 2022, 10.1038/s41388-022-02519-z
- Cell Rep, 2021, 35(1):108940
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S8583 |
Repotrectinib (TPX-0005)
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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 Discov, 2023, 13(3):598-615
- EMBO Mol Med, 2023, 10.15252/emmm.202217367
- Cancer Res, 2022, canres.1397.2021
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S1392 |
Pelitinib (EKB-569)
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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. |
- Cancer Cell, 2022, S1535-6108(22)00312-9
- Cancer Discov, 2022, 12(5):1378-1395
- Cell Oncol (Dordr), 2022, 45(4):601-619
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S1181 |
ENMD-2076
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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
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S8518 |
AD80
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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. |
- Nat Commun, 2022, 13(1):2500
- Mol Cancer Res, 2020, 18(8):1176-1188
- Mol Cancer Res, 2020, 1176-1188
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S2622 |
PP121
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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
- PLoS One, 2016, 11(10):e0164895
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S4921 |
MNS (3,4-Methylenedioxy-β-nitrostyrene)
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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
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S6567 |
Src Inhibitor 1
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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. |
- Sci Adv, 2024, 10(6):eadi4935
- PLoS Biol, 2022, 20(1):e3001518
- Front Cell Dev Biol, 2022, 10:942718
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S7743 |
CCT196969
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CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. |
- Nat Commun, 2022, 13(1):7113
- Cell Rep, 2019, 29(3):573-588
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S8161 |
ON123300
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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
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S0020 |
RK 24466
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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
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S5617 |
Myristic Acid
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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. |
- Nat Commun, 2023, 14(1):660
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S0791 |
eCF506
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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
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S8706 |
UM-164
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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. |
- Cancers (Basel, 2022, 14(215343)
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S3226 |
Dehydroabietic acid
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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. |
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S0918 |
Ginkgolic acid C17:1
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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. |
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S6500 |
KX1-004
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KX1-004 is a non-ATP competitive inhibitor of Src protein tyrosine kinase (Src-PTK; IC50 = 40 µM). |
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S5548 |
7-Hydroxy-4-chromone
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7-Hydroxychromone is an inhibitor of Src kinase with IC50 of <300 μM. |
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S9643 |
DGY-06-116
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DGY-06-116 is an irreversible covalent and selective inhibitor of Src with IC50 of 2.6 nM. |
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S9620 |
Elzovantinib (TPX-0022)
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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. |
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E0814 |
Masitinib mesylate
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Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit with IC50 of 200 nM for human recombinant c-Kit, also inhibits PDGFRα/β with IC50s of 540/800 nM, Lyn with IC50 of 510 nM for LynB, and, to a lesser extent, FGFR3 and FAK. |
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S6060 |
HPK1-IN-2
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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. |
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E2202 |
1-Naphthyl PP1 hydrochloride
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1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively. |
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E2643 |
TL02-59
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TL02-59 is an orally active, selective Src-family kinase Fgr inhibitor with an IC50 of 0.03 nM. |
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S2213 |
AMG-47a
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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. |
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S1272 |
XL228
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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. |
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S9826 |
TPX-0046
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TPX-0046 is a novel RET/SRC inhibitor with a mean IC50 of 17 nM for RETG810R in Ba/F3 cell proliferation assay. |
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S2642 |
1-Naphthyl PP1(1-NA-PP1)
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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. |
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S6383 |
1-NM-PP1
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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. |
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E1634New |
CH6953755
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CH6953755 is a potent, orally active, and selective inhibitor of YES1 kinase with an IC50 of 1.8 nM. CH6953755 demonstrates antitumor activity against YES1 gene-amplified cancers. |
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