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 About 31 results found for searched term "Eg5-IN-1" (0.08 seconds)

Cat.No.  Name Target
M41518 Eg5-IN-1 Kinesin
Eg5-IN-1 is a potent kinesin family motor protein (Eg5) inhibitor with an IC50 value of 1.97 µM.
M1669 Regorafenib VEGFR/PDGFR
BAY 73-4506
Regorafenib (BAY 73-4506) is a novel oral multikinase inhibitor of c-KIT, VEGFR2, B-Raf with IC50s of 17, 40 and 69 nM respectively.
M1964 Vandetanib VEGFR/PDGFR
ZD6474, Zactima
Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase (IC50=40 nM). Vandetanib also inhibited VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM).
M2042 Cilengitide Integrin
EMD 121974, NSC 707544
Cilengitide (EMD 121974, NSC 707544) is a selective inhibitor of αvβ3 integrin and αvβ5 integrin with IC50 of 1 nM and 140 nM, respectively.
M2212 Rociletinib (CO-1686) EGFR/HER2
AVL-301, CNX-419
Rociletinib (CO-1686) is a potent, novel inhibitor of EGFR L858R/T790M kinase with Ki of 21.5 nM and 303.3 nM, respectively.
M2255 Genistein EGFR/HER2
NPI 031L
Genistein is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.
M2595 Raltegravir Integrase
MK-0518
Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.
M3139 ZM 306416 VEGFR/PDGFR
CB 676475
ZM 306416 is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.
M3269 KRN 633 VEGFR/PDGFR
KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.
M3484 Dolutegravir Integrase
GSK1349572
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.
M3684 Canertinib dihydrochloride EGFR/HER2
CI-1033 dihydrochloride, Canertinib 2HCl, PD-183805 dihydrochloride
Canertinib 2HCl is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4.
M4752 l-Chicoric-acid HIV Protease
(-)-Chicoric acid; trans-Caffeoyltartaric acid
L-chicoric Acid ((-)-Chicoric Acid), a dicafoyl tartaric Acid, is a potent, selective and reversible INHIBITOR of HIV-1 integrase with an IC50 of approximately 100 nM. L-chicoric Acid also inhibits HIV-1 replication in tissue cultures.
M4777 Pregnenolone Cannabinoid
Arthenolone; 3β-Hydroxy-5-pregnen-20-one
Pregnenolone (3β -hydroxy-5-pregnen-20-one) is a powerful neurosteroid, and is the major precursor of various steroids, including steroids. Pregnenolone is a specific signaling inhibitor of cannabinoid CB1 receptor.
M4805 BIBX 1382 EGFR/HER2
Falnidamol
BIBX 1382 is a potent, selective inhibitor of EGFR tyrosine kinase (IC50 = 3 nM); displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM).
M4894 Cabozantinib malate VEGFR/PDGFR
XL184;Cabozantinib S-malate
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively.
M4937 Icotinib Hydrochloride EGFR/HER2
BPI-2009H
Icotinib Hcl(BPI-2009H) is a potent and specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC(50) of 5 nM, including it's mutants of EGFR(L858R), EGFR(L861Q), EGFR(T790M) and EGFR(T790M, L858R).
M5329 Motesanib c-Kit
AMG 706
Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret.
M5557 Deferasirox Cytochrome P450 (e.g. CYP17)
CGP-72670, ICL-670
Deferasirox (ICL-670) is an iron chelator that causes iron loss that promotes BclxL downregulation and cell death. Deferasirox (ICL-670) also induced P450 3A4 and inhibited 2C8 and 1A2.
M5852 Lifitegrast Integrin
SAR 1118; Xiidra
Lifitegrast is an antagonist of integrin lymphocyte function associated antigen-1 (LFA-1). The IC50 of Jurkat T cells to icAM-1 was 2.98nM. Lifitegrast blocks the interaction between LFA-1 and ICAM-1, thereby reducing T cell activity and cytokine secretion.
M5925 Regorafenib HCl VEGFR/PDGFR
BAY73-4506 hydrochloride
Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
M6650 Daminozide Histone demethylase
DaminoDaminozide is a plant growth regulator and selective inhibitor of human KDM2/7 histone demethylases, with IC50 values of 0.55, 1.5, and 2.1 μM for PHF8, KDM2A, and KIAA1718, respectively.Daminozide is >100-fold selective for KDM2/7 demethylases compared to other demethylase subfamily members tested. zide is a selective KDM2/7 inhibitor.
M7658 BTA-1 Others
BTA-1 is a probe for β-amyloid aggregates; fluorescent thioflavin-T derivative; exhibits high affinity for amyloid deposits; displays 50-fold higher affinity than thioflavin-T; selectively stains cerebral plaques and cerebrovascular amyloid deposits in the brains of PS1/APP transgenic mice, as well as Aβ fibrils in postmortem brain tissue obtained from AD patients; crosses the blood brain barrier.
M8733 K67 Others
K67 is a specific inhibitor against the interaction between KEAP1 (Kelch-like ECH-associated protein 1) DC (double glycine repeat and C-terminal region) domain and S349-phosphorylated (human Ser349, mouse Ser351) KIR (Keap1-interacting region) of p62/SQSTM1, thereby preventing phospho-p62 from blocking KEAP1-DC and NRF2 (nuclear factor erythroid 2-related factor 2) DLGex motif association.
M11331 UC2288 Mdm2
UC2288 is a novel p21 attenuator with cellular permeability and oral activity (relatively selective activity for P21), based on the structural synthesis of sorafenib. UC2288 down-regulated the expression of P21 mRNA and reduced the level of P21 protein independently of p53, and had little effect on the stability of P21 protein. UC2288 did not inhibit VEGFR2 and Raf kinases, even at 10 μM.
M8758 GW806742X Necroptosis
GW806742X is an ATP site-targeing kinase inhibitor (IC50 in nM = 2/VEGFR2, 15/SRC, 47/C-FMS, 851/GSK3, 9016/ERBB2, 9120/FGFR) with potent antiproliferation activity against cancer cultures (IC50 in nM = 5/HUVEC-v, 424/HUVEC-b, 81/HEF, 453/MDA468, 470/A375P, 693/HT29, 734/PC3), GW806742X is now better known as Compound 1 for its anti-necroptosis activity via affinity interaction with ML
M9094 EG00229 Trifluoroacetate salt VEGFR/PDGFR
EG-00229 Trifluoroacetate
EG00229 Trifluoroacetate is the first small molecule inhibitor of the neuropilin-1 and VEGF-A interaction with an IC50 of inhibition of 8 uM (125I-VEGF binding to PAE/NRP1 cells).
M9540 ODM-203 VEGFR/PDGFR
ODM203
ODM-203 is an orally available inhibitor of VEGFR and FGFR, with IC50s of 26, 9, 5 nM for VEGFR1, VEGFR2 and VEGFR3, and 11, 16, 6, 35 nM for recombinant FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
M9626 Sitravatinib VEGFR/PDGFR
MGCD516; MG516
Sitravatinib (MGCD516) is an orally active receptor tyrosine kinase (RTK) inhibitor. Inhibition of Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, and TRKB at 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, respectively. 29 nM, 5 nM and 9 nM. Sitravatinib alone has a potent antitumor effect and enhances pD-1 blockade activity by promoting the antitumor immune microenvironment.
M10372 Vazegepant hydrochloride CGRP Receptor
Zavegepant, BHV-3500 hydrochloride
Vazegepant (BHV-3500) hydrochloride is a first-in-class, high affinity CGRP receptor antagonist (hCGRP Ki= 0.023 nM). Vazegepant hydrochloride may be useful in the effective treatment of lung inflammation associated with COVID-19.
M10383 Homo-PROTAC cereblon degrader 1 (OUN20985) PROTAC
OUN20985
Homo-PROTAC cereblon degrader 1 (OUN20985) is a potent and efficient cereblon (CRBN) degrader with minimal effects on IKZF1 and IKZF3.
M10683 IMB-301 HIV Protease
IMB-301 is a specific HIV-1 replication inhibitor that binds to hA3G (human APOBEC3G), interrupts the hA3G-Vif interaction and inhibits Vif-mediated degradation of hA3G. IMB-301 inhibits the replication of HIV-1 in H9 cells (IC50=8.63 uM). Human APOBEC3G is a restriction factor that inhibits human immunodeficiency 1 virus (HIV-1) replication.



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