About 31 results found for searched term "And1-IN-1" (0.055 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M43165 | And1-IN-1 | Others |
| And1-IN-1 is a potent And1 inhibitor. | ||
| M1643 | AEE788 | EGFR/HER2 |
| NVP-AEE 788 | ||
| AEE788 (NVP-AEE788) is a novel multitargeted HER 1/2 and VEGFR 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. | ||
| M1676 | BIBR1532 | Checkpoint |
| BIBR-1532 | ||
| BIBR1532 is a potent and selective telomerase inhibitor with IC50 of 100 nM. BIBR 1532 inhibits the proliferation of JVM13 leukemia cells with an IC50 of 52 μM, and similar effect also occurs in other leukemia cell lines such as Nalm-1, HL-60, and Jurkat. BIBR1532 is also an inhibitor of TERT, the rate-limiting enzyme in the regulation of telomerase activity. | ||
| M1694 | CYC116 | Aurora Kinase |
| CYC116 is a potent, small molecule inhibitor of Aurora A, B and C with IC50 value of 44, 19 and 65 nM respectively. CYC-116 also inhibits VEGFR2, Src, Lck AND FLT3 with with Kis of 44, 82, 280, 44 nM, respectively. CYC-116 may have broad-spectrum antitumor activity. | ||
| M1717 | GSK1904529A | IGF-1R |
| GSK1904529A selectively inhibits IGF-IR and IR with IC50s of 27 and 25 nmol/L, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity. | ||
| M1740 | R547 | CDK |
| R547 is a potent and selective ATP-competitive CDK inhibitor, with Ki values of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively. | ||
| M1784 | Icotinib | EGFR/HER2 |
| BPI-2009H | ||
| Icotinib (BPI-2009H) is a potent and novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with an IC50 of 5 nM. Iconitib inhibits the proliferation of A431 and BGC-823 A549, H460 and KB cell lines with IC50s of 1, 4.06, 12.16, 16.08, 40.71 μM. | ||
| M1828 | Tandutinib | FLT3 |
| MLN518, CT53518 | ||
| Tandutinib (MLN518, CT53518) is an orally active multitargeted tyrosine kinase inhibitor of FLT3 (IC50 = 0.22 μM), and it also inhibits c-Kit and PDGFR with IC50 values of 0.17 μM and 0.20 μM, respectively. Tandutinib has the ability to cross the blood-brain barrier. | ||
| M1921 | Mizoribine | DNA/RNA Synthesis |
| Bredinin | ||
| Mizoribine (Bredinin) is an imidazole nucleoside and an immunosuppressive agent with an IC50 of approximately 100 μM. Mizoribine inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively. | ||
| M1942 | Alectinib | ALK |
| CH5424802; AF802 | ||
| Alectinib (CH5424802) is a highly selective, orally active and potent ALK inhibitor with IC50 of 1.9 nM. Alectinib (CH5424802) also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. Alectinib demonstrates effective central nervous system (CNS) penetration. | ||
| M1957 | BMS-536924 | IGF-1R |
| Bms-536924 is an orally active, competitive and selective insulin-like growth factor receptor (IGF-1R) kinase and insulin receptor (IR) inhibitor with IC50 of 100 nM and 73 nM, respectively. It also showed moderate inhibitory activity against Mek, Fak and Lck, but almost no inhibitory activity against Akt1 and MAPK1/2. | ||
| M2022 | Torin 2 | mTOR |
| Torin 2 is a potent and selective mTOR inhibitor with IC50 of 2.1 nM. Torin 2 also inhibits DNA-PK with an IC50 of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2. | ||
| M2028 | Fludarabine | STAT |
| Fludara; NSC 118218; Fludarabinum; F-ara-A | ||
| Fludarabine (NSC 118218) is a STAT1 activation inhibitor and a DNA synthesis inhibitor. Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. Fludarabine markedly inhibited VSMC proliferation in cell culture. Fludarabine also induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Fludarabine exhibits antiproliferative activity (IC50 = 1.54 μM in RPMI cells) and triggers apoptosis through increasing Bax and decreasing Bid, XIAP and survivin expression. | ||
| M2056 | PJ34 hydrochloride | PARP |
| PJ34 hcl | ||
| PJ34 hydrochloride is the hydrochloride form of PJ34, a PARP inhibitor, and inhibits PARP-1-dependent cell death (parthanatos) with an EC50 of 20 nM, acting equally effectively on PARP1/2. | ||
| M2059 | A-922500 | DGAT |
| DGAT-1 Inhibitor 4a; A922500 | ||
| A-922500 (DGAT-1 Inhibitor 4a) is a potent and selective DGAT-1 inhibitor with IC50 values of 9 and 22 nM at human and mouse DGAT-1 respectively. | ||
| M2067 | AGI-5198 | Isocitrate Dehydrogenase (IDH) |
| IDH-C35 | ||
| AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 μM and 0.16 μM, respectively. | ||
| M2071 | ONX-0914 | Proteasome |
| PR-957 | ||
| Onx-0914 (PR-957) is a selective inhibitor of low molecular weight polypeptide 7 (LMP7), a chymotrypsin subunit of the immune proteasome. Onx-0914 blocks cytokine production and reduces the progression of experimental arthritis. Onx-0914 is a non-competitive irreversible inhibitor of mycobacterium proteasome (Ki=5.2 μM). Onx-0914 activates latent HIV-1 through HF-1-mediated p-TEFb activation. | ||
| M2151 | INK128 (Sapanisertib) | mTOR |
| MLN0128; TAK-228 | ||
| INK128 (Sapanisertib; MLN0128) is a potent and selective dual TORC1/2 inhibitor with IC50 of 1 nM. | ||
| M2166 | Birinapant | IAP |
| TL32711 | ||
| Birinapant (TL32711) is a bivalent Smac analogue, which is a potent antagonist of XIAP and cIAP1 with Kd values of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces autoubiquitination and proteasome degradation of cIAP1 and cIAP2 in intact cells, resulting in the formation of RIPK1: Caspase-8 complex, which activates and induces tumor cell death. | ||
| M2204 | T0901317 | Liver X Receptor |
| T0901317 is a potent and selective agonist for both LXRα and LXRβ with an EC50 of 20~50 nM. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. | ||
| M2210 | A-803467 | Sodium Channel |
| A803467 | ||
| A-803467 is a potent and selective Nav1.8 sodium channel blocker that potently blocks tetrodotoxin-resistant currents (IC50 = 140 nM). | ||
| M2218 | Ribociclib (LEE011) | CDK |
| Ribociclib | ||
| Ribociclib (LEE011) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is 1000 times less active against cyclin B/CDK1 complex. | ||
| M2241 | Adapalene | RAR/RXR |
| CD271; Differin; ADA | ||
| Adapalene is a third-generation topical retinoid, it is a potent RAR agonist, with AC50 values of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene is also an MST1 agonist. | ||
| M2276 | Torin 1 | mTOR |
| Torin 1 is a potent and selective inhibitor of mTOR with IC50 of 2 and 10 nM for mTORC1 and mTORC2, respectively. Torin 1 induces cellular autophagy. | ||
| M2294 | Brefeldin A | ATPase |
| BFA; Cyanein; Decumbin | ||
| Brefeldin A is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2 μM in HCT 116 cells. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity. | ||
| M2301 | NVP-TAE226 | FAK |
| TAE226 | ||
| Nvp-tae 226 (TAE226) is a potent atP-competitive dual FAK and IGF-1R inhibitor with IC50 of 5.5 nM and 140 nM, respectively. Nvp-tae 226 (TAE226) also effectively inhibited Pyk2, insulin receptor (InsR), with IC50 of 3.5 nM and 40 nM. | ||
| M2310 | BX-795 | PDK1 |
| BX795 is a potent and specific TBK1, IKKε and PDK-1 inhibitor with IC50 of 6 nM, 41 nM and 111 nM, respectively. | ||
| M2328 | Pirfenidone | TGF-beta/Smad |
| AMR69; S-7701 | ||
| Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone inhibits TGF-β bioactivity by affecting TGF-β2 mRNA expression and processing of pro-TGF-β in CCL-64 cells. Pirfenidone (AMR69) attenuates CCL2 and CCL12 production in fibrocyte cells. | ||
| M2597 | Betrixaban | Factor Xa |
| PRT-054021 | ||
| Betrixaban is a highly potent, selective, and orally efficacious factor Xa inhibitor with IC50 of 1.2 nM(inhibition of Factor 10a). | ||
| M2381 | AMD3465 hexahydrobromide (AMD3465 ) | CXCR |
| GENZ-644494 hexahydrobromide | ||
| AMD3465 hexahydrobromide（AMD3465 ) is an effective CXCR4 antagonist that inhibits 12G5 mAb in SupT1 cells. The IC50 values of CXCL12AF647 and CXCR4 were 0.75 nM and 18 nM, respectively. AMD 3465 also effectively inhibited X4 HIV replication (IC50, 1-10 nM), but not R5 HIV replication. | ||
| M2383 | AMG-517 | TRP Channel |
| AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM. | ||
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