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Src
Src Products
- All (49)
- Src Inhibitors (48)
- Src Activator (1)
- New Src Products
| Catalog No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| S1021 | Dasatinib | Dasatinib 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S7060 | PP1 | PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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). | ||
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| S7743 | CCT196969 | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S0791 | eCF506 | eCF506 is a potent, selective and orally bioavailable inhibitor of Src tyrosine kinase with IC50 < 0.5 nM. | ||
| S8321 | Tolimidone (MLR-1023) | Tolimidone (MLR-1023) 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. | ||
| 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. | ||
| 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. | ||
| E4630New | Ilginatinib hydrochloride | Ilginatinib hydrochloride (NS-018 hydrochloride) is a potent small-molecule inhibitor of JAK2 that is competitive with adenosine triphosphate (ATP) which exhibits 30–50-fold greater selectivity for JAK2 over other Jak-family kinases such as JAK1, JAK3, and TYK2.It inhibits JAK2, JAK1, JAK3, and TYK2 with IC50 of 0.72 nM, 33 nM, 39 nM, and 22 nM, respectively. It also showed potent inhibition of Src-family kinases, SRC and FYN. It can be used in research of myeloproliferative neoplasms. | ||
| 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 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| 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. |
|
|
| S7060 | PP1 | PP1 (AGL 1872, EI 275) is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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). | ||
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| 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. |
|
|
| 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. |
|
|
| 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. | ||
| S7743 | CCT196969 | CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| S0791 | eCF506 | eCF506 is a potent, selective and orally bioavailable inhibitor of Src tyrosine kinase with IC50 < 0.5 nM. | ||
| 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. | ||
| 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. | ||
| E4630New | Ilginatinib hydrochloride | Ilginatinib hydrochloride (NS-018 hydrochloride) is a potent small-molecule inhibitor of JAK2 that is competitive with adenosine triphosphate (ATP) which exhibits 30–50-fold greater selectivity for JAK2 over other Jak-family kinases such as JAK1, JAK3, and TYK2.It inhibits JAK2, JAK1, JAK3, and TYK2 with IC50 of 0.72 nM, 33 nM, 39 nM, and 22 nM, respectively. It also showed potent inhibition of Src-family kinases, SRC and FYN. It can be used in research of myeloproliferative neoplasms. | ||
| 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. |
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| 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. | ||
| S8321 | Tolimidone (MLR-1023) | Tolimidone (MLR-1023) 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. | ||
| E4630New | Ilginatinib hydrochloride | Ilginatinib hydrochloride (NS-018 hydrochloride) is a potent small-molecule inhibitor of JAK2 that is competitive with adenosine triphosphate (ATP) which exhibits 30–50-fold greater selectivity for JAK2 over other Jak-family kinases such as JAK1, JAK3, and TYK2.It inhibits JAK2, JAK1, JAK3, and TYK2 with IC50 of 0.72 nM, 33 nM, 39 nM, and 22 nM, respectively. It also showed potent inhibition of Src-family kinases, SRC and FYN. It can be used in research of myeloproliferative neoplasms. | ||
| 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. |
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