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Lck Inhibitor is a small-molecule inhibitor. It takes participate in the T-cell receptor (TCR) signal transduction and affects the expression of genes associated with cell proliferation, cytokine release and T-cell survival. It has been designed and developed as therapeutic agents for the treatment for T-cell-mediated autoimmune and organ transplant rejection. It showed high selectivity against Lck over another Src family kinase Src and the kinases. It also showed more than 1000-fold greater selectivity over CDK, MAPK and the RSK family. Synonyms: TC-S 7003; TC S 7003; TCS 7003; TC-S-7003; TCS7003; TCS-7003. Grades: >98%. CAS No. 847950-09-8. Molecular formula: C31H30N8O. Mole weight: 530.62.
Lck inhibitor 2
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. It inhibited 48 kinases with control less than 1%(33 of them tyrosine kinases, almost half of the 71 tyrosine kinases in the panel). Synonyms: Benzamide, 3-[[4-[(5-hydroxy-2-methylphenyl)amino]-2-pyrimidinyl]amino]-. Grades: >98%. CAS No. 944795-06-6. Molecular formula: C18H17N5O2. Mole weight: 335.36.
Lck Inhibitor - CAS 213743-31-8
The Lck Inhibitor, also referenced under CAS 213743-31-8, controls the biological activity of Lck. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. Group: Fluorescence/luminescence spectroscopy.
2,3-Dimethylbutyl Chloroformate
2,3-Dimethylbutyl Chloroformate is used to prepare phenyl (piperazinylphenyl) pyrazolo[1, 5-a]pyrimidinylamine derivatives for use as Lck inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 1215109-12-8. Pack Sizes: 1g, 10g. Molecular Formula: C7H13ClO2, Molecular Weight: 164.63. US Biological Life Sciences.
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(2-Bromo-4-pyridinyl)-boronic Acid
(2-Bromo-4-pyridinyl)-boronic Acid is a reagent used to prepare Lck inhibitors. Group: Biochemicals. Grades: Highly Purified. CAS No. 458532-94-0. Pack Sizes: 1g, 5 g. Molecular Formula: C5H5BBrNO2, Molecular Weight: 201.81. US Biological Life Sciences.
KP372-1 is a specific Akt inhibitor that demonstrates at least 10-fold selectivity against a panel of additional kinase targets, including CDK1, ERK1, GSK3β, LCK, MEK1, PKA, PKC, and S6K. It blocks Akt signalling through the PI3K pathway, and inhibits cell proliferation while inducing apoptosis of thyroid cancer cells. Synonyms: 6H-Indeno[1,2-e]tetrazolo[1,5-b][1,2,4]triazin-6-one. Grades: ≥95%. CAS No. 1374996-60-7. Molecular formula: C20H8N12O2. Mole weight: 448.4.
A 419259
A-419259 is a potent inhibitor of Src family kinases. IC50 values for src, lck, blk, csk, fyn and lyn range between 15 and 50 nM. Synonyms: A419259; A-419259; RK 20449; RK20449; RK-20449. Grades: >98%. CAS No. 364042-47-7. Molecular formula: C29H34N6O. Mole weight: 482.62.
A cell-permeable furopyrimidine that acts as a potent, ATP-binding site-targeting, Ack1-selective inhibitor (IC50 = 22nM) and effectively prevents receptor-mediated Ack1 activation (by >90% in MEF & LAPC4 cultures; 16h 800nM), while exhibiting much reduced potency against Lyn, Lck, Abl1 and BTK (IC50 ≥346.7nM) and no inhibitory activity toward 25 other kinases. Shown to completely inhibit EGF-induced, but not androgen DHT- (dihydrotestosterone) stimulated, AR transcription activity in serum- and androgen-deprived prostate cancer LAPC4 cutlures. Effectively inhibits androgen-independent LNCaP prostate cancer growth both in vitro (by 60%; 72h 8uM) and in castrated mice in vivo (4mg/kg/96h injections on day 7/11/15/19/23/27 post tumor transplant). Group: Biochemicals. Grades: Highly Purified. CAS No. 873305-35-2. Pack Sizes: 10mg. US Biological Life Sciences.
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AMG-47a
AMG-47a is a potent inhibitor of Lck and T cell proliferation. It has anti-inflammatory activity (ED50 = 11 mg/kg) in the anti-CD3 induced production of IL-2 in mice. It displays subnanomolar inhibition against Lck, and low inhibition against other hard to inhibit kinases in several other in vitro assays. It effectively inhibits the JNK family of kinases including TYK2 at ~ 1.2 μM but well under 10 μM. It selectively reduced the levels of EGFP-KRASG12V protein but did not affect EGFP protein in cells. Uses: Amg-47a has anti-inflammatory activity. Synonyms: AMG-47a; AMG 47a; AMG47a; AMG-47; AMG 47; AMG47. 4-Methyl-3-[2-[[2-(4-morpholinyl)ethyl]amino]-6-quinazolinyl]-N-[3-(trifluoromethyl)phenyl]benzamide. Grades: 95%. CAS No. 882663-88-9. Molecular formula: C29H28F3N5O2. Mole weight: 535.56.
Anomalin A
Lck (p56lck; lymphocyte specific tyrosine kinase) inhibitor. Antioxidant. DPPH radical scavenger. Group: Biochemicals. Alternative Names: 2,3,6,8-Tetrahydroxy-1-methylxanthone. Grades: Highly Purified. CAS No. 548740-86-9. Pack Sizes: 1mg. Molecular Formula: C14H10O6. US Biological Life Sciences.
Worldwide
Anomalin A (2,3,6,8-Tetrahydroxy-1-methylxanthone)
Originally isolated from the marine fungus Arthrinium sp., Anomalin A is a potent Lck (p56lck; lymphocyte specific tyrosine kinase) inhibitor. Also acts as an antioxidant and DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenger. Group: Biochemicals. Grades: Highly Purified. CAS No. 548740-86-9. Pack Sizes: 1mg. US Biological Life Sciences.
Worldwide
ATR Kinase Inhibitor II (3-Amino-6-(4-((1-(dimethylamino)propan-2-yl)sulfonyl)-phenyl)-N-phenylpyrazine-2-carboxamide)
A cell-permeable aminopyrazinyl-sulfone compound that acts as a potent, reversible and ATP-competitive inhibitor of ATR kinase (IC50 = 12nM; Ki=6nM) with excellent selectivity over ATM, DNA-PK (IC50 > 8uM) and in a 50-kinase panel (% inhibition at 2uM = 59, 57, 55, 52, 43 and 42 for AMPK, Lck, RIPK2, Ret, IKK-alpha and FGFR3, respectively). Shown to block pH2AX-Ser139 (IC50 = 420nM in hydroxyurea treated HT29 cells) and preferentially enhance cisplatin cytotoxicity against tumor cells over normal cells by ~7-fold at 620nM. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??N?O?S. US Biological Life Sciences.
A cell-permeable quinazoline compound that targets the ATP binding pocket and an adjacent cleft and acts as a potent and reversible inhibitor of Aurora A and Aurora B (IC50=110 and 130nM, respectively) with moderate to excellent selectivity among closely related 16-kinase panel (IC50=0.88, 1.03 and 1.79uM for Lck, Src and MEK1, respectively, and IC50>10uM for Cdk1/2/4, Plk1, Chk1). Blocks phosphorylation of Histone H3-Ser10 in Xenopus cycling egg extracts at 20uM, and reduces mitotic spindle assembly. Shown to repress kinetochore localization of BubR1, Cenp-E, and Mad2, and arrest the growth of proliferating tumor cells. Group: Biochemicals. Grades: Highly Purified. CAS No. 331771-20-1. Pack Sizes: 5mg. US Biological Life Sciences.
Worldwide
BMS-243117
BMS-243117 is a potent and selective Lck inhibitor with good cellular activity against T-cell proliferation. BMS-24311 has potential to treat diseases such as rheumatoid arthritis and asthma. Synonyms: BMS-243117; BMS 243117; BMS243117; UNII-MBE6KWV0QI; CHEMBL67237; MBE6KWV0QI; SCHEMBL6058200. 2-(tert-butylcarbamoylamino)-N-(2-chloro-6-methylphenyl)-1,3-benzothiazole-6-carboxamide; BMS-243117; UNII-MBE6KWV0QI. Grades: >98%. CAS No. 225521-80-2. Molecular formula: C20H21ClN4O2S. Mole weight: 416.92.
BMS358233
BMS358233 is a potent Lck inhibitor. It has excellent cellular activities against T-cell proliferation. Uses: Bms358233 has excellent cellular activities against t-cell proliferation. Synonyms: BMS-358233; BMS 358233; 6-Benzothiazolecarboxamide, N-(2-chloro-6-methylphenyl)-2-((6-methyl-2-((((2R)-tetrahydro-2-furanyl)methyl)amino)-4-pyrimidinyl)amino)-. Grades: 98%. CAS No. 601519-75-9. Molecular formula: C25H25ClN6O2S. Mole weight: 509.02.
BMS 599626 dihydrochloride
BMS 599626 dihydrochloride is a potent and selective EGFR and ErbB2 inhibitor (IC50 = 22 nM and 32 nM, respectively), and also inhibits HER4 (IC50 = 190 nM). BMS 599626 displays 100-fold selectivity for EGFR and ErbB2 over VEGFR2, c-Kit, Lck, MET etc MEK and Lck. It can be used as an antiproliferative agent in vitro and anti-tumorigenic agent in vivo. Synonyms: BMS599626 dihydrochloride; BMS-599626 dihydrochloride; AC480 dihydrochloride; AC 480 dihydrochloride; AC-480 dihydrochloride; (3S)-3-Morpholinylmethyl-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamate dihydrochloride; Carbamic acid, N-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-, (3S)-3-morpholinylmethyl ester, hydrochloride (1:2); (3S)-3-Morpholinylmethyl (4-{[1-(3-fluorobenzyl)-1H-indazol-5-yl]amino}-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate dihydrochloride. Grades: ≥98% by HPLC. CAS No. 1781932-33-9. Molecular formula: C27H27FN8O3.2HCl. Mole weight: 603.48.
BMS-599626 Hydrochloride
BMS-599626 Hydrochloride (AC480 Hydrochloride) is a selective and orally bioavailable HER1 and HER2 inhibitor, with IC 50 s of 20 and 30 nM, respectively. BMS-599626 Hydrochloride displays ~8-fold less potent to HER4 (IC 50=190 nM), >100-fold to VEGFR2, c-Kit, Lck, MEK. BMS-599626 Hydrochloride inhibits tumor cell proliferation, and has potential to increase tumor response to radiotherapy [1] [2]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AC480 Hydrochloride. CAS No. 873837-23-1. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-12010.
BMS 777607
BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met , Axl , Ron and Tyro3 with IC 50 s 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 [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: BMS 817378. CAS No. 1025720-94-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-12076.
CGP77675
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src ( IC 50 s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC 50 s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 234772-64-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-W062835.
Damnacanthal
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC 50 s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans [1] [2] [3] [4]. Uses: Scientific research. Group: Natural products. CAS No. 477-84-9. Pack Sizes: 1 mg; 5 mg. Product ID: HY-108485.
Dasatinib Monohydrate
Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, PDGFR, ephrin receptors, Src, c-Kit, and other Src-family kinases (LCK, HCK, FYN, and others). Uses: Antineoplastic agents. Synonyms: BMS-354825 Monohydrate; BMS 354825 Monohydrate; BMS354825 Monohydrate; N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide hydrate. Grades: >98%. CAS No. 863127-77-9. Molecular formula: C22H28ClN7O3S. Mole weight: 506.02.
Fostamatinib
Fostamatinib (R788) is the oral proagent of the active compound R406 [1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a K i of 30 nM and an IC 50 of 41 nM [2]. R406 also inhibits Lyn (IC 50 =63 nM) and Lck (IC 50 =37 nM) [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: R788. CAS No. 901119-35-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13038A.
Fostamatinib Disodium
Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406 [1]. R406 is an orally available and competitive Syk/FLT3 inhibitor with a K i of 30 nM and an IC 50 of 41 nM [2]. R406 also inhibits Lyn (IC 50 =63 nM) and Lck (IC 50 =37 nM) [3]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: R788(Disodium). CAS No. 1025687-58-4. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13038.
An orally bioavailable and blood-brain-barrier permeable oxadiazolo-benzofuranyl phenyl sulfoxide compound that acts as a potent, reversible and ATP-competitive inhibitor of GSK-3b (IC50=35nM, 34 and 140nM for racemic, (S)-9b eutomer and (R)-9b distomer). The (S)-9b eutomer displays excellent selectivity (IC50 > 10uM) over Cdk1/2/5, Chk1, p38a, JNK1, MEKK1, IKKb, PKCth, CK1d, EGFR, ErbB2, Src, Lck, IR, Tie2, c-Kit, c-Met, VEGFR2, FGFR3 and PDGFRa/b, and lowers tau phosphorylation at GSK-3b-Thr205 in a CWS (cold water stress) mouse model (3mg/kg, p.o.). Group: Biochemicals. Grades: Highly Purified. CAS No. 1005201-24-0. Pack Sizes: 5mg. US Biological Life Sciences.
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JNJ-26483327
JNJ-26483327 is an orally bioavailable, small-molecule, multitargeted reversible tyrosine kinase inhibitor with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor JNJ-26483327 binds to and inhibits several members of the epidermal growth factor receptor (EGFR) family, including EGFR, HER2 and HER4; Src family kinases (Lyn, Yes, Fyn, Lck and Src); and vascular endothelial growth factor receptor type 3 (VEGFR3). By inhibiting several different signaling molecules that play crucial roles at various stages in tumorigenesis, this agent may inhibit tumor growth, invasion, migration and metastasis. In addition, JNJ-26483327 crosses the blood-brain barrier (BBB). Synonyms: JNJ-26483327; JNJ 26483327; JNJ26483327. CAS No. 807640-87-5. Molecular formula: C22H25BrN4O2. Mole weight: 457.372.
Kenpaullone - CAS 142273-20-9
A potent, cell-permeable, and reversible inhibitor of glycogen synthase kinase-3? (IC?? = 230 nM), Lck (IC?? = 470 nM), and cyclin-dependent kinases (Cdks). Group: Fluorescence/luminescence spectroscopy.
LCKLSL
LCKLSL is a competitive inhibitor of annexin A2 (AnxA2). It can effectively inhibit the binding of tissue plasminogen activator (tPA) and AnxA2. It can also inhibit the production of plasmin and has an anti-angiogenic effect. Synonyms: LCKLSL; HY-P2333; AKOS040758181; 533902-29-3; CS-0130051. CAS No. 533902-29-3. Molecular formula: C30H57N7O8S. Mole weight: 675.88.
LDC1267
LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8. Synonyms: LDC1267; LDC 1267; LDC-1267. Grades:>98%. CAS No. 1361030-48-9. Molecular formula: C30H26F2N4O5. Mole weight: 560.55.
Masitinib
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit ( IC 50 =200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β ( IC 50 s=540/800 nM), Lyn ( IC 50 = 510 nM for LynB), Lck , and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity [1] [2] [4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AB1010. CAS No. 790299-79-5. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-10209.
Masitinib mesylate
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit ( IC 50 =200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β ( IC 50 s=540/800 nM), Lyn ( IC 50 = 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 [1] [2] [4]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AB-1010 mesylate. CAS No. 1048007-93-7. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg; 200 mg. Product ID: HY-10209A.
NG25
Type II inhibitor of TAK1 (MAP3K7) and MAP4K2 (GCK) with nanomolar potency for a wider range of kinases (IC50 values 13 nM, 22 nM, 56 nM, 75 nM, 82 nM, 102 nM, 113 nM, and 149 nM for LYN, MAP4K2, CSK, Abl, FER, p38α, SRC, and TAK1, repectively). At 0.1 μM NG25 shows strong inhibition of TAK1, Lck, MAP4K2, p38α, Abl, YES1, and OSR1. NG 25 potently inhibited the activation of IKKβ by TLR7 and TLR9 agonists and prevented the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells. Synonyms: NG 25; NG-25. Grades: >98%. CAS No. 1315355-93-1. Molecular formula: C29H30F3N5O2. Mole weight: 537.58.
NG 25 trihydrochloride
NG 25 trihydrochloride is a type II inhibitor of TAK1 (MAP3K7) and MAP4K2 (GCK) with nanomolar potency for multiple kinases including TAK1, Lck, MAP4K2, p38α, Abl, YES1, and OSR1. NG 25 potently inhibits the activation of IKKβ by TLR7 and TLR9 agonists, and prevents the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells. Synonyms: NG 25 trihydrochloride; NG25 trihydrochloride; NG-25 trihydrochloride. Grades: 98%. CAS No. 2108554-00-1. Molecular formula: C29H30F3N5O2.3HCl. Mole weight: 646.96.
OSI-930
OSI-930 is an orally selective inhibitor of Kit , KDR and CSF-1R (c-Fms) with IC 50 s 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 [1]. Uses: Scientific research. Group: Signaling pathways. CAS No. 728033-96-3. Pack Sizes: 10 mM * 1 mL; 1 mg; 5 mg; 10 mg; 50 mg. Product ID: HY-10204.
Poloxipan
Poloxipan is a potent and pan-specific PLK1 inhibitor. In vitro, Poloxipan has IC50 3.2 uM (Plk1); 1.7 uM (Plk2); and 3 uM (Plk3). Poloxipan showed minor inhibition over FHA dommain of Chk2, S2 domian of STAT1, STAT5b, Lck, etc. Synonyms: (Z)-2-(5-bromo-2-methoxybenzylidene)-6-methyl-2H-thiazolo[3,2-b][1,2,4]triazine-3,7-dione; 2-(5-Bromo-2-methoxybenzylidene)-6-methyl-2H-thiazolo[3,2-b][1,2,4]triazine-3,7-dione. Grades: 98%. CAS No. 1239513-63-3. Molecular formula: C14H10BrN3O3S. Mole weight: 380.22.
PP1
PP1 is a potent, and Src family-selective tyrosine kinase inhibitor with IC 50 of 5 and 6 nM for Lck and Fyn, respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AGL 1872; EI 275. CAS No. 172889-26-8. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13804.
PP1 Analog IV, 3-IB-PP1 (3-Iodobenzyl PP1 Analog)
A cell-permeable enlarged PP1 analog that acts as a potent, ATP-competitive and reversible inhibitor of asAkt1/2/3 (IC50=28, 240 and 120nM, respectively) over wtAkt1/2/3 (IC50= >10uM). Shown to hyperphosphorylate Akt-Ser473 and -Thr308 in HEK293 cells coexpressed with myr-HA-asAkt1 or myr-HA-asAkt1/2/3 with no effect on pGSK-3bSer9 levels and wtAkt expressing cells. Also, specifically blocks the inhibitory function of membrane asCsk with diminished activity towards wtCsk, induces phosphorylation of Lck-Tyr394 and ERK1/2 in primary mouse T cells (EC50 ~0.5uM) and rapidly activates T cell receptor signaling. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C16H18IN5, Molecular Weight: 407.3. US Biological Life Sciences.
Worldwide
PP2
PP2, also known as AG 1879, is a substance that has frequently been used in cancer research as a "selective" inhibitor for Src-family kinases. It strongly inhibits the kinases Lck (IC50=4 nM), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of EGFR (480 nM) and practically no inhibition of ZAP-70 (100 μM) and JAK2 (50 μM). Despite its extensive use as a Src-selective inhibitor, recent research has shown that PP2 is non-selective and inhibits many other kinases with similar affinities. Uses: Designed for use in research and industrial production. Additional or Alternative Names: PP2; PP-2; PP 2; AG 1879; AG-1879; AG1879. Product Category: Inhibitors. Appearance: Solid powder. CAS No. 172889-27-9. Molecular formula: C15H16ClN5. Mole weight: 301.77. Purity: >98%. IUPACName: 1-(tert-butyl)-3-(4-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine. Canonical SMILES: NC1=C2C(N(C(C)(C)C)N=C2C3=CC=C(Cl)C=C3)=NC=N1. Product ID: ACM172889279. Alfa Chemistry ISO 9001:2015 Certified.
PP2
PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC 50 s of 4 and 5 nM for Lck and Fyn , respectively. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AGL 1879. CAS No. 172889-27-9. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-13805.
RK-20448
RK-20448 is the cis-isomer of A-419259. RK-20448 acts as an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R, and Tie-2 (IC50s = 0.24, 1.19, 10.74, and 5.85 μM, respectively). Synonyms: 7-[4-(4-methylpiperazin-1-yl)cyclohexyl]-5-(4-phenoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine. Grades: ≥98%. CAS No. 479501-40-1. Molecular formula: C29H34N6O. Mole weight: 482.62.
RK-24466
RK-24466 is a cell-permeable and ATP-competitive inhibitor of lymphocyte-speci?c protein tyrosine kinase (Lck). It was shown to suppress cell receptor-stimulated IL-2 production in mice. Synonyms: Lck Inhibitor?; 4-Amino-5-(4-Phenoxyphenyl)-7H-Pyrrolo[2,3-D]pyrimidin-7-yl-Cyclopentane; 7-Cyclopentyl-5-(4-phenoxy)phenyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamine. Grades: ≥95%. CAS No. 213743-31-8. Molecular formula: C23H22N4O. Mole weight: 370.5.
Saracatinib
Saracatinib (AZD0530) is a potent Src family inhibitor with IC 50 s 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 [1]. Uses: Scientific research. Group: Signaling pathways. Alternative Names: AZD0530. CAS No. 379231-04-6. Pack Sizes: 10 mM * 1 mL; 5 mg; 10 mg; 50 mg; 100 mg. Product ID: HY-10234.
SPP 86
SPP 86 is a potent and cell-permeable RET inhibitor (IC50 = 8 nM). It also inhibits EphA1, FGFR1, Flt4, Lck and Yes. SPP 86 suppresses the proliferation of HCT 116 and TPC1 cells in vitro. Synonyms: SPP-86; SPP 86; SPP86; 1-(1-Methylethyl)-3-(2-phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine; 3-(2-phenylethynyl)-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-4-amine. Grades: ≥98% by HPLC. CAS No. 1357349-91-7. Molecular formula: C16H15N5. Mole weight: 277.32.
Src I1
Src I1 is a dual site inhibitor that competes at both the ATP and peptide binding sites of Src tyrosine kinase (IC50 = 44 and 88 nM for Src and Lck, respectively). Src I1 was reported to inhibit VEGFR2 and c-fms at higher concentrations (IC50 = 0.32 and 30 μM, respectively). Synonyms: Src I1; Src I-1; SrcI1. 6,7-Dimethoxy-N-(4-phenoxyphenyl)-4-quinazolinamine; Src Kinase Inhibitor I; Src Inhibitor 1; Src Inhibitor-1. Grades: ≥99% by HPLC. CAS No. 179248-59-0. Molecular formula: C22H19N3O3. Mole weight: 373.4.
STAT5-IN-1
STAT5-IN-1, a cell-permeable nonpeptidic nicotinoyl hydrazone compound, is a selective STAT5 inhibitor with an IC50 of 47 μM for STAT5β isoform with much less effect towards the SH2 domain of STAT1, STAT3, or Lck (IC50>500 μM). Synonyms: MDK-6314; STAT5 Inhibitor; STAT5Inhibitor; STAT5-Inhibitor; MDK 6314; MDK6314. N-[(E)-(4-oxochromen-3-yl)methylideneamino]pyridine-3-carboxamide; STAT5 Inhibitor. CAS No. 285986-31-4. Molecular formula: C16H11N3O3. Mole weight: 293.28.
TG 100801
TG 100801 is a proagent that generates TG 100572 by de-esterification in development to treat age-related macular degeneration. TG 100572 is a multi-targeted kinase inhibitor which inhibits receptor tyrosine kinases and Src kinases ; has IC 50 s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1 , VEGFR2 , FGFR1 , FGFR2 , PDGFRβ , Fgr , Fyn , Hck , Lck , Lyn , Src , Yes , respectively. Uses: Scientific research. Group: Signaling pathways. CAS No. 867331-82-6. Pack Sizes: 5 mg; 10 mg; 25 mg; 50 mg; 100 mg. Product ID: HY-10186.
WH-4-023
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 values of 2 nM and 6 nM for Lck and Src kinase respectively. In combination with PD 0325901, CHIR99021 and SB-590885, WH-4-023 was found to support self-renewal of naive human embryonic stem cells (hESCs). Synonyms: KIN001-112; KIN112; 2,6-dimethylphenyl (2,4-dimethoxyphenyl)(2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)carbamate. Grades: >98%. CAS No. 837422-57-8. Molecular formula: C32H36N6O4. Mole weight: 568.67.
A cell-permeable diphenylpyrazolo compound that disrupts HIV accessary protein Nef dimerization (IC50 = 3uM in HEK293T cells) and prevents Nef-mediated Src family kinase Hck activation (IC50 = 2.8uM) without directly affecting the catalytic activity of c-Src, Hck, Lck, or Lyn. Shown to suppress HIV and SIV viral replication (IC50/strain/culture = 1uM/SIV deltaB670/CEM-174 and <0.3uM/HIV-1 NL4-3/CEM-T4) and infectivity, being ineffective against the replication of Nef-defective HIV-1 mutant. Molecular docking and in vitro binding studies reveal a high-affinity B9-targeting site formed at the Nef dimerization interface and a low-affinity binding site on each Nef monomer at the dimer interface periphery. Group: Biochemicals. Grades: Highly Purified. Pack Sizes: 10mg. Molecular Formula: C??H??ClN?O?S, Primary Target: Nef. US Biological Life Sciences.
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