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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
137 Results for "
LCK
" in MedChemExpress (MCE) Product Catalog:
Products (137)
137 Results for "LCK" in MCE Product Catalog:
626
626 Publications Verification
Synonyms: SB 203580; RWJ 64809
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
626
626 Publications Verification
Synonyms: SB 203580 hydrochloride; RWJ 64809 hydrochloride
Adezmapimod (SB 203580; RWJ 64809) hydrochloride is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod hydrochloride inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod hydrochloride does not disrupt JNK activity and is an autophagy and mitophagy activator .
64
43
Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases .
43
43 Cited Publications
Synonyms: AZD0530 difumarate
Saracatinib (AZD0530) difumarate is a potent Src inhibitor with IC50 values of 2.7-11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr and Blk, and is selective for other tyrosine kinases. .
37
37 Cited Publications
Research Areas:
R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
37
37 Cited Publications
Research Areas:
R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation . R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
17
17 Cited Publications
Synonyms: Src Kinase Inhibitor 1; Src-l1
Src Inhibitor 1 is a potent, ATP-competitive and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
16
Research Areas:
Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
16
16 Cited Publications
Synonyms: R788Disodium
Research Areas:
Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
16
16 Cited Publications
Synonyms: R788 disodium hexahydrate
Research Areas:
Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
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12
Target:
Research Areas:
BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases .
11
A 419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, has high selectivity towards the Src family. A 419259 shows inhibitory effect for Src, Lck and Lyn with IC50 of 9 nM, <3 nM and <3 nM, respectively .
11
7
7 Cited Publications
Target:
Research Areas:
A-770041 is a selective and orally active Src-family Lck inhibitor. A-770041 inhibits Lck with an IC50 value of 147 nM with the presence of 1 mM ATP. A-770041 shows 300-fold selective to Lck over Fyn, the other Src family kinase involved in T-cell signaling. A-770041 can be used for the research of acute rejection .
6
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity .
6
6 Cited Publications
Synonyms: AB-1010 mesylate
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity .
5
5 Cited Publications
Synonyms: 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; little inhibition on p38α and KDR.
4
4 Cited Publications
OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
