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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