| DC75043 |
Tipiracil HCl |
Tipiralacil, also known as TPI, is a thymidine phosphorylase inhibitor (TPI). Tipiracil is one of the active components in TAS-102, which is an anticancer drug candidate currently in clinical trials. TAS-102 consists of the cytotoxin Trifluridine and the thymidine phosphorylase inhibitor (TPI) tipiracil. Trifluridine is incorporated into DNA during DNA synthesis and inhibits tumor cell growth. Tipiracil protects trifluridine from being broken down when taken orally. TAS-102 was approved in Japan in 2015. |
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| DC75044 |
GGTI-298 free base |
GGTI-298 is a potent geranylgeranyltransferase-I (GGTase-I) inhibitor with potential antitumor actrivity. GGTI-298 disrupts MAP kinase activation and G(1)-S transition in Ki-Ras-overexpressing transformed adrenocortical cells. GGTI-298 induces hypophosphorylation of retinoblastoma and partner switching of cyclin-dependent kinase inhibitors. A potential mechanism for GGTI-298 antitumor activity. GGTI-298 arrests human tumor cells in G0/G1 and induces p21(WAF1/CIP1/SDI1) in a p53-independent manner. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells. |
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| DC75045 |
BMS-1166 free base |
BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor. BMS-1166 binds to human PD-L1 and blocks its interaction with PD-1. BMS-1166 alleviates the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes. Moreover, BMS-1166 was effective in attenuating the inhibitory effect of the cell surface-associated PD-L1. |
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| DC75046 |
Azalanstat HCl |
Azalanstat is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg/kg/day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg/kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1. |
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| DC75047 |
Umbralisib |
Umbralisib, also known as TGR1202 and RP5264 , is a highly specific, orally available, PI3K delta inhibitor, targeting the delta isoform with nanomolar potency and several fold selectivity over the alpha, beta, and gamma isoforms of PI3K. Inhibition of PI3K delta signaling with TGR-1202 has demonstrated robust activity in numerous pre-clinical models and primary cells from patients with hematologic malignancies. |
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| DC75048 |
Gemcitabine monophosphate disodium salt |
Gemcitabine monophosphate disodium salt, also called GemMP, is a monophosphate derivative of Gemcitabine. Gemcitabine (Gem) is a deoxycytidine analog that is effective against pancreatic cancer and other malignancies following conversion to the 5'-O-mono-, di- and tri-phosphate forms. GemMP decreased tumor cell growth at concentrations ranging from 1 to 50 nM. GemMP is a potent cytotoxic agent that serves to induce apoptosis in association with increased Fas expression in cultured thyroid cancer cell lines. (Anticancer Res. 2000 Sep-Oct;20(5A):2915-22). Note: Current batch has purity ~ 90%. |
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| DC75049 |
PF-04929113 free base |
PF-04929113, also known as SNX-5422; is a synthetic prodrug targeting the human heat-shock protein 90 (Hsp90) with potential antineoplastic activity. Although the mechanism of action remains to be fully elucidated, Hsp90 inhibitor SNX-5542 is rapidly converted to SNX-2112, which accumulates in tumors relative to normal tissues. SNX-2112 inhibits Hsp90, which may result in the proteasomal degradation of oncogenic client proteins, including HER2/ERBB2, and the inhibition of tumor cell proliferation. |
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| DC75050 |
ASP2905 free base |
ASP2905 hydrochloride is a potent and selective inhibitor of the potassium voltage-gated channel subfamily H member 3 (KCNH3). |
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| DC75051 |
ASN007 free base |
ASN007, a novel oral ERK inhibitor, shows robust antitumor activity in RAS mutant cancer models. with low single-digit nM IC50 values. ASN007 showed a slow dissociation rate (long target residence time) as compared to several other known ERK inhibitors. In mechanistic cell-based assays, ASN007 inhibited the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines. ASN007 showed single-digit nanomolar antiproliferative activity that was selective for MAPK-pathway dependent cancer cell lines. |
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| DC75052 |
FTI-2148 free base |
FTI-2148 is a potent farnesyltransferase inhibitor with potential antitumor activity. FTI-2148 is highly selective for FTase (IC50, 1.4 nM) over GGTase I (IC50, 1700 nM). FTI-2148 suppressed the growth of the human lung adenocarcinoma A-549 cells in nude mice by 33, 67, and 91% in a dose-dependent manner. Combination therapy of FTI-2148 with either cisplatin, gemcitabine, or Taxol resulted in a greater antitumor efficacy than monotherapy. |
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| DC75053 |
JNJ-63576253 |
JNJ63576253, also known as TRC253, is a potent and orally active androgen receptor antagonist. TRC253 specifically binds to both wild-type and certain mutant forms of AR, thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot translocate to the nucleus. This prevents binding to and transcription of AR-responsive genes, inhibits the expression of genes that regulate prostate cancer cell proliferation, and may lead to an inhibition of growth of tumor cells in which AR is overexpressed and/or mutated. AR is often overexpressed and/or mutated in prostate cancers and plays a key role in proliferation, survival and chemoresistance of tumor cells. |
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| DC75054 |
Vactosertib |
Vactosertib, also known as TEW-7197 is a potent ALK5 inhibitor. TEW-7197 showed potent in vivo anti-metastatic activity, indicating its potential for use as an anti-cancer therapy. EW-7197 inhibits TGF-β/Smad signaling. EW-7197 abrogates TGF-β1-induced tumor cell migration and invasion. EW-7197 inhibits breast cancer metastasis to the lung.EW-7197 prolongs the life span of BALB/c 4T1 mice via inhibition of EMT. EW-7197 inhibits metastasis and enhances the activity of cytotoxic T lymphocytes (CTLs) in 4T1 orthotopic grafted mice. |
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| DC75055 |
SHR1653 |
SHR1653 is a highly potent and selective oxytocin receptor (OTR) antagonist with improved blood-brain barrier penetration, which might be beneficial for the treatment of CNS-related PE. |
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| DC75056 |
Chlorthenoxazine |
Chlorthenoxazine is a non-steroidal anti-inflammatory drug (NSAID). |
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| DC75057 |
Saracatinib free base |
Saracatinib, also known as AZD0530, is an orally available dual-specific inhibitor of Src and Abl with anti-invasive and anti-tumor activities. Src and Abl are protein tyrosine kinases that are overexpressed in chronic myeloid leukemia cells. Saracatinib binds to and inhibits these tyrosine kinases and their effects on cell motility, cell migration, adhesion, invasion, proliferation, differentiation, and survival. |
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| DC75058 |
SRT-1720 HCl |
SRT-1720, also known as CAY10559 and is a drug developed by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. It has similar activity in the body to the known SIRT1 activator resveratrol, but is 1000x more potent. In animal studies it was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increased mitochondrial and metabolic function. A study of SRT1720 conducted by the National Institute on Aging found that the drug may extend the lifespan of obese mice by 44% . |
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| DC75059 |
CX-6258 |
CX-6258 is a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity. CX-6258 exhibited in vitro synergy with chemotherapeutics and robust in vivo efficacy in two Pim kinases driven tumor models. Inhibition of Pim kinases is expected to have a beneficial effect as cancer therapy. |
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| DC75060 |
CR8 hydrochloride |
CR8 is a potent and selective inhibitor of CDK. CR8 is a more potent pyridyl analogue of roscovitine. In comparison to roscovirtine, the compound gains in potency toward CK1, which is involved in amyloid-β formation. The R-CR8 enantiomer is slightly more potent than S. CR8 is around 30 times more potent at cellular assay then roscovitine. |
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| DC75061 |
PF-06446846 HCl |
PF-06446846 is a selective orally active PCSK9 inhibitor that appears to act by causing the ribosome to stall when synthesizing PCSK9. PCSK9 binds to the LDL receptor, preventing it from removing LDL cholesterol from the blood. PF-06446846 was found to reduce plasma PCSK9 and total cholesterol levels in rats. |
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| DC75062 |
GSK2814338 free base |
GSK2814338, also known as Lp-PLA2 -IN-1, is a Lp-PLA2 inhibitor |
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| DC75063 |
PHA-767491 free base |
PHA 767491 hydrochloride is a potent and selective ATP-competitive dual inhibitor cdc7/cdk9. PHA-767491 blocks DNA synthesis and affects the phosphorylation of the replicative DNA helicase at Cdc7-dependent phosphorylation sites. |
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| DC75064 |
K-604 HCl |
K-604 is a potent and selective acyl-CoA:cholesterol acyltransferase 1 (ACAT-1) inhibitor. K-604 inhibits against acyl-coenzyme A (acyl-CoA):cholesterol O-acyltransferase-1 (ACAT1, SOAT1) activitiy in a selective (IC50 = 450 nM vs. 102.85 μ M against human ACAT1 and ACAT2, respectively) and acyl-CoA-competitive (Ki = 378 nM against oleoyl-coA) manner. |
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| DC75065 |
Avitriptan HCl |
Avitriptan, also known as BMS-180048, is a selective 5-HT1-like receptor agonist. Avitriptan is an effective compound for the treatment of migraine headaches with a prolonged duration of response. Avitriptan Is a Ligand and Agonist of Human Aryl Hydrocarbon Receptor That Induces CYP1A1 in Hepatic and Intestinal Cells. |
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| DC75066 |
Rolapitant HCl |
Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. |
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| DC75067 |
Atevirdine |
Atevirdine, also known as U-87201, is a non-nucleoside reverse transcriptase inhibitor that has been studied for the treatment of HIV. Atevirdine has been shown to have significant anti-HIV RT activity in vitro, it inhibits HIV-1 replication in infected peripheral blood leukocyte cultures at a 50% inhibitory concentration of 1 nM and a concentration which is cytotoxic to 50% of cells of 100 μM and also inhibits completely the formation of syncytia in human T-cell leukemia virus type III-infected MT-2 cells at 2 μM. |
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| DC75068 |
Antalarmin |
Antalarmin is a CRF-1 antagonist. By blocking CRF-1 activity the release of ACTH is reduced, and chronic stress is decreased in response to chronic stress. Antalarmin could be useful in reducing the adverse health consequences of chronic stress in humans, as well as treating anxiety, depression, and drug addiction. |
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| DC75069 |
BS-181 HCl |
BS-181 is a highly selective CDK inhibitor for CDK7 with an IC(50) of 21 nmol/L. Testing of other CDKs as well as another 69 kinases showed that BS-181 only inhibited CDK2 at concentrations lower than 1 micromol/L, with CDK2 being inhibited 35-fold less potently (IC(50) 880 nmol/L) than CDK7. In MCF-7 cells, BS-181 inhibited the phosphorylation of CDK7 substrates, promoted cell cycle arrest and apoptosis to inhibit the growth of cancer cell lines, and showed antitumor effects in vivo. |
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| DC75070 |
AZ-505 TFA |
AZ505 is a potent and highly selective inhibitor of SMYD2 with potential anticancer activity. AZ505 is composed of three distinct moieties: benzooxazinone, cyclohexyl, and dichlorophenethyl substituents. The structure of the ternary complex reveals that a single AZ505 molecule is bound in the peptide binding groove of SMYD2. |
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| DC75071 |
Obatoclax mesylate |
Obatoclax, also known as GX 015-070, a synthetic small-molecule inhibitor of the bcl-2 family of proteins with potential pro-apoptotic and antineoplastic activities. Obatoclax binds to members of the Bcl-2 protein family, preventing the binding of these anti-apoptotic proteins to the pro-apoptotic proteins Bax and Bak and so promoting the activation of the apoptotic pathway in Bcl-2-overexpressing cells. The Bcl-2 family of proteins (bcl-2, bcl-xl, bcl-w, and Mcl-1) are overexpressed in a wide variety of cancers, including those of the lymphatic system, breast, lung, prostate, and colon. |
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| DC75072 |
AZ505 free base |
AZ505 is a potent and highly selective inhibitor of SMYD2 with potential anticancer activity. AZ505 is composed of three distinct moieties: benzooxazinone, cyclohexyl, and dichlorophenethyl substituents. The structure of the ternary complex reveals that a single AZ505 molecule is bound in the peptide binding groove of SMYD2. |
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