| 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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| DC75073 |
BGP-15 HCl |
BGP-15 is a novel poly(ADP-ribose) polymerase inhibitor - protects against nephrotoxicity of cisplatin without compromising its antitumor activity. BGP-15 also inhibits caspase-independent programmed cell death in acetaminophen-induced liver injury. Moreover, BGP-15 was found to prevent imatinib-induced cardiotoxicity by activating Akt and suppressing JNK and p38 MAP kinases. |
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| DC75074 |
Allitinib tosylate |
Allitinib, also known as AST1306 and ALS 1306, is a potent, selective, irreversible ErbB2 and EGFR inhibitor. AST-1306 inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 was found to function as an irreversible inhibitor, most likely through covalent interaction with Cys797 and Cys805 in the catalytic domains of EGFR and ErbB2, respectively. In vivo, AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models, but weakly inhibited the growth of EGFR-overexpressing tumor xenografts. |
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| DC75075 |
BAY 61-3606 |
BAY 61-3606 is a potent (Ki = 7.5 nM) and selective inhibitor of Syk kinase. BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606. |
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| DC75076 |
UAMC-3203 HCl |
UAMC-3203 is a Ferroptosis Inhibitor wtih IC50 = 12 nM. UAMC-3203 showed an improved protection compared to Fer-1 against multiorgan injury in mice. No toxicity was observed in mice after daily injection of UAMC-3203 for 4 weeks. UAMC-3203 inserts rapidly in a phospholipid bilayer in silico, which aligns with the current understanding of the mechanism of action of these compounds. In conclusion, these analogues have superior properties compared to Fer-1, show in vivo efficacy, and represent novel lead compounds with therapeutic potential in relevant ferroptosis-driven disease models. |
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| DC75077 |
BSJ-03-123 HCl |
BSJ-03-123 is a potent, CDK6-selective small-molecule degrader (PROTAC). Pharmacologic CDK6 degradation targets a selective dependency of acute myeloid leukemia cells, and transcriptomics and phosphoproteomics profiling of acute degradation of CDK6 enabled dynamic mapping of its immediate role in coordinating signaling and transcription. |
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| DC75078 |
FLX925 (AMG-925) |
FLX925, also known as AMG-925, is a potent and selective type 1 inhibitor of FLT3 that retains its cellular potency against clinically relevant secondary resistance mutations in FLT3 occurring with quizartinib or sorafenib treatment (FLX925 IC50: MOLM13ITD, 15 nM; MOLM13ITD/D835, 28 nM; MV4-11ITD, 16 nM; MV4-11ITD/D835, 19 nM; MV4-11ITD/N841, 16 nM; MV4-11ITD/F691, 73 nM). |
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| DC75079 |
Elacestrant HCl |
Elacestrant, also known as RAD1901, is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. Upon oral administration of higher doses of RAD1901, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells. At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss. In addition, RAD1901 is able to cross the blood-brain barrier (BBB). |
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| DC75080 |
Tamatinib free base |
Tamatinib, also known as R406, is a potent inhibitor of immunoglobulin E (IgE)- and IgG-mediated activation of Fc receptor signaling (EC(50) for degranulation = 56-64 nM). The primary target for R406 is the spleen tyrosine kinase (Syk). R406 inhibited phosphorylation of Syk substrate linker for activation of T cells in mast cells and B-cell linker protein/SLP65 in B cells. R406 bound to the ATP binding pocket of Syk and inhibited its kinase activity as an ATP-competitive inhibitor (K(i) = 30 nM). |
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| DC75081 |
Quizartinib HCl |
Quizartinib, also known as AC220 and AC010220, is a highly potent FMS-like receptor tyrosine kinase-3 (FLT3) inhibitor. Quizartinib HCl inhibits FLT3 activity and displays antitumor properties in a mouse MV4-11 tumor xenograft model. |
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| DC75082 |
Bimiralisib free base |
Bimiralisib, also known as PQR309, is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy. |
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| DC75083 |
Neratinib |
Neratinib, also known as HKI-272 or PB272, is an orally available, irreversible inhibitor of the HER-2 receptor tyrosine kinase with potential antineoplastic activity. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocket of the receptor. |
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| DC75084 |
Xaliproden HCl |
Xaliproden, also known as SR57746, is a drug which acts as a 5HT1A agonist. It has neurotrophic and neuroprotective effects in vitro, and has been proposed for use in the treatment of several neurodegenerative conditions including amyotrophic lateral sclerosis and Alzheimer's disease. The SR57746A activates PI3-K/AKT- and ERK-signaling in IECs. Depending on ERK- and AKT activation, SR57746A potently prevents apoptosis of IECs without inducing proliferation or migration in these cells. Moreover, SR57746A prevented apoptosis in EGCs in vitro. Topical SR57746A treatment significantly reduced mucosal injury in 2 experimental murine colitis models and was as effective as intraperitoneal infliximab treatment. |
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| DC75085 |
Ensartinib free base |
Ensartinib, also known as X-396, is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. |
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| DC75086 |
Defactinib free base |
Defactinib, also known as VS-6063 and PF-04554878, is an orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. |
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| DC75087 |
Peficitinib free base |
Peficitinib, also known as ASP015K and JNJ-54781532, is a novel potent JAK inhibitor, which demonstrated potent efficacy in adjuvant-induced arthritis model in rats. ASP015K inhibited JAK1, JAK2, JAK3 and TYK2 enzyme activities with IC50 values of 3.9, 5.0, 0.71 and 4.8 nM, respectively. ASP015K inhibited the IL-2-induced proliferation of human T cells with an IC50value of 18 nM. Moreover, ASP015K was 14-fold more potent against JAK1/3 than JAK2/2 on the basis of EPO-induced proliferation of human leukemia cells. |
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| DC75088 |
PD-153035 free base |
PD153035 is a ATP-competitive EGFR inhibitor with an IC50 and Ki of 25 and 6 pM. PD153035 effectively blocks the enhancement of mitogenesis, induction of early gene expression, and oncogenic transformation that occur in response to EGF receptor stimulation. With human fibroblasts and epidermoid carcinoma cells, PD153035 at nanomolar concentrations rapidly inhibits EGFR autophosphorylation. With breast and ovarian cancer cells, PD153035 not only blocks cell growth via inhibition of EGFR, but also upregulates the expression of the tumor suppressor retinoic acid receptor-beta 2 (RAR-beta2). |
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| DC75089 |
Palifosfamide-Tris |
Palifosfamide, also known as ZIO201, is a synthetic mustard compound with potential antineoplastic activity. An active metabolite of ifosfamide covalently linked to the amino acid lysine for stability, palifosfamide irreversibly alkylates and cross-links DNA through GC base pairs, resulting in irreparable 7-atom inter-strand cross-links; inhibition of DNA replication and cell death follow. Unlike ifosfamide, this agent is not metabolized to acrolein or chloroacetaldehyde, metabolites associated with bladder and CNS toxicities. In addition, because palifosfamide does not require activation by aldehyde dehydrogenase, it may overcome the tumor resistance seen with ifosfamide. |
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| DC75090 |
AV-412 Tosylate |
AV-412, also known as MP-412, is a second-generation, orally bioavailable dual kinase inhibitor with potential antineoplastic activity. EGFR/HER2 inhibitor AV-412 binds to and inhibits the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor 2 (HER2), which may result in the inhibition of tumor growth and angiogenesis, and tumor regression in EGFR/HER2-expressing tumors. This agent may be active against EGFR/HER2-expressing tumor cells that are resistant to first-generation kinase inhibitors. EGFR and HER2 are receptor tyrosine kinases that play major roles in tumor cell proliferation and tumor vascularization. |
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| DC75091 |
Pacritinib (SB1518) |
Pacritinib, also known as SB1518, is an orally bioavailable inhibitor of Janus kinase 2 (JAK2) and the JAK2 mutant JAK2V617F with potential antineoplastic activity. Pacritinib competes with JAK2 for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and so caspase-dependent apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders; the JAK2V617F gain-of-function mutation involves a valine-to-phenylalanine modification at position 617. The JAK-STAT signaling pathway is a major mediator of cytokine activity. |
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| DC75092 |
LXH254 free base |
Naporafenib, also known as LXH254, is an orally available inhibitor of all members of the serine/threonine protein kinase Raf family, with potential antineoplastic activity. Upon administration, pan-RAF inhibitor LXH254 binds to Raf proteins and inhibits Raf-mediated signal transduction pathways. This inhibits proliferation of Raf-overexpressing tumor cells. Raf protein kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are upregulated in a variety of cancer cell types. |
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| DC75093 |
Cediranib free base |
Cediranib, also known as AZD-2171, is a potent and selective VEGF inhibitor with antineoplastic activities. Competing with adenosine triphosphate, cediranib binds to and inhibits all three vascular endothelial growth factor receptor (VEGF-1,-2,-3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth. |
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| DC75094 |
Rucaparib Camsylate |
Rucaparib camsylate is a potent, orally available inhibitor of poly ADP-ribose polymerase (PARP) 1 and 2. |
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