Src

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Src	Lck	Fyn	Lyn	Yes	Other
A10290	Dasatinib	****					Abl,c-Kit (D816V),c-Kit (wt)
A10108	Saracatinib	***	***	**	***		EGFR (L861Q),c-YES,EGFR (L858R)
A10161	Bosutinib	****					Abl
A11177	KX2-391	**
A10661	NVP-BHG712	*					EphB4,C-Raf,c-Abl
A12723	PP2	***	***	***			EGFR
A12724	PP1	***	***	**			Kit,EGFR,Bcr-Abl
A15518	SU6656	*		*	*	*
A16320	Dasatinib Monohydrate	****					Abl ,c-Kit (D816V),c-Kit (wt)
A14117	WH-4-023	****	****
A10766	Quercetin						Sirtuin,PKC,PI3Kγ
A11288	A-770041		*
A12417	MLR 1023				**
A13232	1-NA-PP1	****		****			c-Abl, CDK2, CAMK II
A13415	MCB-613	***	****		****
A13819	TG 100801	****		****			VEGFR1, VEGFR2, FGFR1
A13820	TG 100572	****		****			VEGFR1, VEGFR2, FGFR1
A13868	PD 166285						FGFR1, PDGFRβ, Wee1
A16241	AZM475271	****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No.	Product Name	Application	Product Information
A14117 SALE	WH 4-023	dual Lck/Src inhibitor	WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively.
A12214 SALE	KX1-004	Src-PTK inhibitor	KX1-004 is a potent small molecule inhibitor of Src-PTK as a potential protective drug for NIHL.
A13868	PD-166285	Src inhibitor	PD 166285 is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1).
A15060	Dasatinib hydrochloride	Src inhibitor	Dasatinib hydrochloride is a potent and dual Abl/ Src inhibitor IC50 of ??1 nM/0.8 nM respectively; also inhibit c-Kit (WT)/c-Kit (D816V) with IC50 of 79 nM/37 nM.
A15260	TG 100572 HCl	VEGFR2/Src kinase inhibitor	TG 100572 is a multi-targeted kinase inhibitor that inhibit select growth factor receptor tyrosine kinases and Src familt kinases with IC50 values of 2/7/2/1/0.5 nM for VEGFR1/VEGFR2/FGFR1/Src/Fyn kianse respectively.
A15518 SALE	SU6656	SRC inhibitor	SU6656 is a selective inhibitor of Src kinases, Including Src, Yes, Lyn, and Fyn (IC50 = 280, 20, 130, 170 nM, respectively).
A11471	KX2-391 2HCl	Src inhibitor	KX2-391 2Hcl is 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.
A13415	MCB-613	SRC stimulator	MCB-613 is a potent, pan steroid receptor coactivator (SRC) stimulator.
A11288	A-770041	Lck inhibitor	A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
A14323	A419259	Src inhibitor	A419259 trihydrochloride is an apoptosis inducing agent that inhibits Src family kinases (c-Src).
A10161 SALE	Bosutinib (SKI-606)	Src inhibitor	Bosutinib (SKI-606) is a tyrosine kinase inhibitor undergoing research for use in the treatment of cancer. Product Citations (1) Matthew S. Zabriskie, etc. BCR-ABL1 Compound Mutations Combining Key Kinase Domain Positions Confer Clinical Resistance to Ponatinib in Ph Chromosome-Positive Leukemia. Cancer Cell. 2014 Sep 8; 26(3): 428–442.
A16240	MNS	Src/Syk inhibitor	MNS is a potent and selective inhibitor of Src and Syk tyrosine kinases.
A16241	AZM475271	Src inhibitor	AZM475271 is a potent and selective Src kinase inhibitor with IC50 of 5 nM; no inhibitory activity on Flt3, KDR, Tie-2.
A16244	T338C Src-IN-2	Src inhibitor	T338C Src-IN-2 is a potent mutant c-Src T338C kinase inhibitor with IC50 of 317 nM; also inhibits T338C/V323A and T338C/V323S with IC50 of 57 nM/19 nM.
A16243	T338C Src-IN-1	Src inhibitor	T338C Src-IN-1 is a potent mutant-Src T338C inhibitor; exhibited the most potent inhibition of T338C(IC50=111 nM) relative to WT c-Src (10-fold increase).
A15140	Lck Inhibitor	Lck Inhibitor	Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.
A15141	Lck inhibitor 2	Lck inhibitor	Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively .
A16242	CPDA	SHIP2 inhibitor	CPDA is a novel potent SHIP2 inhibitor that can effectively ameliorate insulin resistance in 3T3-L1 adipocytes.
A16086	Tilfrinib	Brk inhibitor	Tilfrinib is a potent and selective breast tumor kinase (Brk) inhibitor (IC50 = 3.15 nM).
A12234	Scutellarein	-	Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
A10108 SALE	Saracatinib (AZD0530)	Src/Abl inhibitor	Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively. Product Citations (3) Chisato Naito,et al. Facilitatory effects of fetuin-A on atherosclerosis, Atherosclerosis, 2016, Mar;246:344-51 26828753 Kenta Maruyama,et al. 5-Azacytidine-induced Protein 2 (AZI2) Regulates Bone Mass by Fine-tuning Osteoclast Survival, J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 25691576 Amanda L Jackson,et al. Emerging therapies: angiogenesis inhibitors for ovarian cancer, Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 26001052
A10290 SALE	Dasatinib (BMS-354825)	Abl-Src inhibitor	Dasatinib (BMS-354825) is an oral multi- BCR/ABL and Src family tyrosine kinase inhibitor. The main targets of dasatinib, are BCR/ABL, Src, c-Kit, ephrin receptors, and several other tyrosine kinases, but not erbB kinases such as EGFR or Her2. Product Citations (5) Sano T,et al. Gliding Basal Cell Migration of the Urothelium during Wound Healing, Am J Pathol, 2018, Nov;188(11):2564-2573 30121259 Ines Peschel,et al. FLT3 and FLT3-ITD phosphorylate and inactivate the cyclin-dependent kinase inhibitor p27Kip1 in acute myeloid leukemia, Haematologica, 2017, Aug; 102(8): 1378-1389 28522571 Brittany M. Duggan,et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 28484277 John D. Leonard,et al. Identification of natural regulatory T cell epitopes reveals convergence on a dominant autoantigen, Immunity, 2017, Jul 18; 47(1): 107-117.e8. 28709804 Fujita KI,et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 28479358
A10661 SALE	NVP-BHG712	EphB4 inhibitor	NVP-BHG712 is a selective inhibitor of EphB4 kinase that exhibits selectivity for EphB4 over more than 40 other kinases in vitro, including FGFR3.
A10766 SALE	Quercetin (Sophoretin)	MAO-B inhibitor	Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
A11177 SALE	KX2-391	Src inhibitor	KX2-391 is a novel non-ATP competitive substrate-pocket directed SRC inhibitor.
A11207 SALE	PP121	PI3K Inhibitor	PP121 is a dual inhibitor of receptor tyrosine kinases (RTKs) (IC50 < 0.02 μM for Abl, Src, VEGFR-2 and PDGFR) and PI 3-K family kinases (IC50 < 0.06 μM for p110α, DNA-PK and mTOR).
A12417 SALE	MLR 1023	-	MLR 1023 is a selective allosteric activator of Lyn kinase (EC50 = 63 nM)
A12724 SALE	PP1	Src Inhibitor	PP1 is a potent inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 5 and 6 nM respectively). Displays > 8000-fold selectivity over ZAP-70 and JAK2. Also moderately inhibits p38, CSK, PDGF receptors, RET-derived oncoproteins, c-Kit and Bcr-Abl
A12723 SALE	PP2	Src Inhibitor	PP2 is a selective inhibitor of Src-family tyrosine kinases. Inhibits p56lck and p59fynT (IC50 values are 4 and 5 nM respectively). Displays > 10000-fold selectivity over ZAP-70 and JAK2. Moderately inhibits CSK (IC50 = 0.73 μM).
A13069 SALE	XL-228	IGF-1R, Aurora, FGFR, ABL, SRC inhibitor	XL228 is a protein kinase inhibitor targeting IGF1R, the AURORA kinases, FGFR1-3, ABL and SRC family kinases. XL228 is an Aurora A inhibitor (IC50, f3 nmol/L) that has shown potent biochemical activity against ABL1 (Ki, 5 nmol/L), as well as the BCR-ABL1 T315I (Ki, 1.4 nmol/L) kinases.
A13232 SALE	1-NA-PP1	Src Kinase inhibitor	1-NA-PP1 is a selective inhibitor of v-Src and c-Fyn as well as c-Abl
A13167 SALE	AMG-47a	Lck inhibitor	AMG-47a is an orally bioavailable potent inhibitor of Lck and T cell proliferation. It exhibits anti-inflammatory activity (ED50 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice.
A13573 SALE	PP1 Analog II, 1NM-PP1	-	PP1 Analog II, 1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors.
A13821	CGP77675	Src inhibitor	CGP77675 is a potent Src kinase inhibitor. CGP77675 inhibited phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50: 5-20 and 40 nM, respectively).
A13820	TG 100572	VEGFR2/Src inhibitor	TG 100572 is VEGFR2 and Src kinase inhibitor.
A13819	TG 100801	VEGFR2/Src inhibitor	TG 100801 is a VEGFR2 targeting prodrug currently in a clinical trial. The active form is TG100572.
A13290	A-419259	SFK inhibitor	A-419259 is an inhibitor of Src family kinases (SFK) (IC50 = 0.1 - 0.3 uM).
A16265	Lyn-IN-1	dual Bcr-Abl/Lyn inhibitor	Lyn-IN-1 is a potent and selective dual Bcr-Abl/Lyn inhibitor, extracted from patent WO2014169128A1.

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A14117 SALE

A12214 SALE

A13868

A15060

A15260

A15518 SALE

A11471

A13415

A11288

A14323

A10161 SALE

A16240

A16241

A16244

A16243

A15140

A15141

A16242

A16086

A12234

A10108 SALE

A10290 SALE

A10661 SALE

A10766 SALE

A11177 SALE

A11207 SALE

A12417 SALE

A12724 SALE

A12723 SALE

A13069 SALE

A13232 SALE

A13167 SALE

A13573 SALE

A13821

A13820

A13819

A13290

A16265

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