Oxazinanes
Medchemexpress LLC Thz1 (hydrochloride) | 99.1% | C31H29Cl2N7O2 | 10MM/1ML
THZ1 Hydrochloride is a selective and potent covalent inhibitor of CDK7, with an IC50 of 3.2 nM. It also inhibits the closely related kinases CDK12 and CDK13, leading to the downregulation of MYC expression.
- Functions as a selective and potent covalent CDK7 inhibitor.
- Inhibits closely related kinases, specifically CDK12 and CDK13.
- Downregulates MYC expression.
Medchemexpress LLC Prexasertib (dihydrochloride) | 1234015-54-3 | 99.4% | 438.31 | 5 MG
Prexasertib dihydrochloride (LY2606368 dihydrochloride) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. It also inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). This compound causes double-stranded DNA breakage and replication catastrophe leading to apoptosis and shows potent anti-tumor activity.
- Selective ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor.
- Inhibits CHK2 and RSK1.
- Causes double-stranded DNA breakage and replication catastrophe.
- Leads to apoptosis and potent anti-tumor activity.
- Induces growth inhibition in tumor xenografts.
- Inhibits CHK1 in blood.
- Promotes phosphorylation of H2AX (S139) and RPA2 (S4/S8).
- Associated with clinical trials for various neoplasms.
Apexbio Technology LLC CBL0137 (hydrochloride) 1197397-89-9 2mg
CBL0137 (hydrochloride) (CAS 1197397-89-9) is a small-molecule curaxin that modulates transcriptional regulation by targeting the Facilitates Chromatin Transcription (FACT) complex This interaction leads to activation of p53 (EC50 0 37 M) and inhibition of NF- B signaling (EC50 0 47 M) pathways commonly dysregulated in cancer In vitro CBL0137 induces apoptosis in pancreatic cancer cell lines affecting both differentiated tumor cells and cancer stem cells In vivo studies demonstrate antitumor activity in models resistant to gemcitabine with additional combinatory effects attributed to transcriptional inhibition CBL0137 is under clinical evaluation in solid and hematological malignancies
Medchemexpress LLC HXR9 hydrochloride | 99.5% | 2754.67 | 1 MG
HXR9 hydrochloride is a cell-permeable peptide that acts as a competitive antagonist of HOX/PBX interaction. It selectively decreases cell proliferation and promotes apoptosis in cells with high HOXA/PBX3 gene expression, such as MLL-rearranged leukemic cells, by blocking the interaction between HOX and PBX transcription factors.
- Antagonizes the interaction between HOX and PBX transcription factors.
- Selectively decreases cell proliferation.
- Promotes apoptosis in cells with high HOXA/PBX3 gene expression.
- Appears as a white to off-white solid.
- Soluble in water (H2O) and PBS.
TARGETMOL CHEMICALS INC MIDODRINE HYDROCHLORIDE 25MG
Also available in 5 mg 10 mg 50 mg 100 mg 1 mL 10 mM (in DMSO) and bulk. Please contact Fisher for quotes. Midodrine is converted to its active metabolite desglymidodrine by deglycination reaction. Desglymidodrine selectively binds to and activates alpha-1-adrenergic receptors of the arteriolar and venous vasculature. This causes smooth muscle contraction and leads to an elevation of blood pressure. Desglymidodrine diffuses poorly across the blood-brain barrier and is therefore not associated with effects on the central nervous system. Midodrine hydrochloride (Pro-Amatine) is the hydrochloride salt form of midodrine a direct-acting prodrug and sympathomimetic agent with antihypotensive properties. purity: 99%
Medchemexpress LLC Prexasertib (dihydrochloride) | 1234015-54-3 | 99.4% | 438.31 | 1 ML
Prexasertib dihydrochloride is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. It causes double-stranded DNA breakage and replication catastrophe, leading to apoptosis, and exhibits potent anti-tumor activity. It also inhibits CHK2 and RSK1.
- Selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor.
- Causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis.
- Shows potent anti-tumor activity.
- Inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM).
Medchemexpress LLC Febrifugine dihydrochloride | 32434-42-7 | MFCD27978373 | 100.0% | 374.26 g/mol | C16H21Cl2N3O3 | 10 MG
Febrifugine dihydrochloride is a quinazolinone alkaloid research compound supplied as the dihydrochloride salt. It exhibits antimalarial activity by inhibiting Plasmodium falciparum and has reported antiproliferative effects in bladder cancer models; provided as a high-purity solid for in vitro and in vivo research.
- Antimalarial activity against Plasmodium falciparum.
- Mechanism involves increased eIF2α phosphorylation leading to parasite inhibition.
- High purity as provided by manufacturer (99.95%).
- White to off-white solid formulation, stable when stored frozen and protected from moisture and light.
- Supplied in small research pack sizes suitable for in vitro and in vivo studies, including 10 mg packs.
Medchemexpress LLC Bomedemstat dihydrochloride | 99.55% | 592.54 | 25 MG
Bomedemstat dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. It increases H3K4 and H3K9 methylation, which then alters gene expression. This compound exhibits anti-cancer activities by inhibiting cancer cell proliferation and inducing apoptosis, and is being investigated in multiple clinical trials.
- Selectively inhibits proliferation of Jak2V617F cells
- Induces apoptosis via BCL-XL and PUMA in a TP53-dependent manner
- Leads to cell cycle arrest in SET-2 cells
- Normalizes or improves blood cell counts in Mx-Jak2V617F mice
- Reduces spleen volumes and restores normal splenic architecture in animal models
Apexbio Technology LLC Dequalinium Chloride 522-51-0 250mg
Dequalinium Chloride (CAS 522-51-0) is a small molecule inhibitor known to target protein kinase C (PKC) with reported IC50 values between 7 18 M PKC is a serine/threonine kinase involved in calcium- and lipid-dependent signaling pathways critical for cell growth and transformation Dequalinium Chloride also acts as a selective blocker of apamin-sensitive potassium channels exhibiting an IC50 of 1 1 M and inhibits angiotensin II-induced K loss (IC50 1 5 M) Notably dequalinium accumulates in mitochondria of cancer cells disrupts mitochondrial enzymes and impairs cellular energy production ultimately leading to cell death It has been used in studies of apoptosis mitochondrial function and as an adjunct in tumor models investigating sensitization to agents such as TNF
Medchemexpress LLC 7,8-Dihydro-L-biopterin | 6779-87-9 | 99.79% | 239.23 | 100 MG
7,8-Dihydro-L-biopterin is a NOS uncoupling inducer that can cross the blood-brain barrier. It is a reduced non-conjugated pteridine and the main metabolite of 4-amino-tetrahydro-L-biopterin, which undergoes photooxidation to form biopterin. This compound promotes the conversion of nitric oxide synthase to a superoxide-producing form, leading to increased oxidative stress in the renal outer medulla and inducing apoptosis.
- NOS uncoupling inducer
- Can cross the blood-brain barrier
- Promotes conversion of nitric oxide synthase to a superoxide-producing form
- Increases oxidative stress in the renal outer medulla
- Induces apoptosis
- Sensitive to inhibitory effect of SOD
- Used in research related to salt-sensitive hypertension and neurodegenerative diseases
Medchemexpress LLC Cl097 (hydrochloride) | 2990770-48-2 | 100.0% | 1 ML
CL097 hydrochloride is a potent agonist for Toll-like Receptor 7 (TLR7) and Toll-like Receptor 8 (TLR8). It induces the production of pro-inflammatory cytokines in macrophages and also triggers NADPH oxidase priming, which leads to an increase in fMLF-stimulated ROS production. This product is provided as a 10 mM solution in DMSO, suitable for various research applications.
- Potent agonist for Toll-like Receptor 7 and 8
- Induces pro-inflammatory cytokines in macrophages
- Triggers NADPH oxidase priming
- Provided as a 10 mM solution in DMSO
- Suitable for research use
Medchemexpress LLC Febrifugine dihydrochloride | 32434-42-7 | 1 MG
Febrifugine dihydrochloride is a quinazolinone alkaloid with antimalarial activity against *P. falciparum*. It also shows anticancer properties in bladder cancer by inhibiting DNA synthesis, inducing apoptosis, and reducing steroids, leading to G1 phase increase and G2 phase decrease in cancer cells. Its action involves suppressing DNA synthesis and promoting apoptosis via downregulating key steroidogenesis factors.
- Inhibits *P. falciparum*.
- Possesses antimalarial activity.
- Inhibits bladder cancer cell proliferation.
- Induces apoptosis in bladder cancer cells.
- Reduces steroid synthesis in bladder cancer cells.
- Increases eIF2α phosphorylation in *P. falciparum*.
- Increases G1 phase cells and decreases G2 phase cells in bladder cancer.
- Significantly reduces mortality and parasitemia in an animal model of malaria.
- Effectively inhibits bladder cancer xenograft proliferation in mice.
Medchemexpress LLC Ipatasertib dihydrochloride | 1396257-94-5 | C24H34Cl3N5O2 | 200 MG
Ipatasertib dihydrochloride is a highly selective and ATP-competitive pan-Akt inhibitor, with IC50s of 5, 18, and 8 nM for Akt1, Akt2, and Akt3 respectively. It demonstrates potent efficacy in xenograft models where Akt is activated due to genetic alterations, leading to tumor growth delay, stasis, or regression. This compound is intended for research use only.
- Highly selective and ATP-competitive pan-Akt inhibitor.
- IC50s of 5, 18, and 8 nM for Akt1, Akt2, and Akt3.
- Significant selectivity for Akt1 compared to closely related kinases.
- Effective in xenograft models with Akt activation due to genetic alterations.
- Induces tumor growth delay, stasis, or regression in vivo.
- Enhances tumor regression and stasis when used in combination therapies.
- Increases tumor growth inhibition in ovarian cancer models when combined with other agents.
Medchemexpress LLC Bomedemstat dihydrochloride | 99.6% | 592.54 | 50 MG
Bomedemstat dihydrochloride is an orally active and irreversible lysine-specific demethylase 1 (LSD1) inhibitor. It increases H3K4 and H3K9 methylation to alter gene expression, showing anti-cancer activities by inhibiting cancer cell proliferation and inducing apoptosis.
- Orally active.
- Irreversible LSD1 inhibitor.
- Increases H3K4 and H3K9 methylation.
- Alters gene expression.
- Exhibits anti-cancer activities.
- Inhibits cancer cell proliferation.
- Induces apoptosis.
- Selectively inhibits proliferation and induces apoptosis of Jak2V617F cells.
- Enhances cell survival and induces apoptosis via BCL-XL and PUMA.
- Leads to cell cycle arrest.
- Normalizes or improves blood cell counts in animal models.
- Reduces spleen volumes in animal models.
- Restores normal splenic architecture.
- Reduces bone marrow fibrosis in animal models.
Medchemexpress LLC Prexasertib (dihydrochloride) | 1234015-54-3 | 99.7% | 438.31 | 50 MG
Prexasertib dihydrochloride is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with potent anti-tumor activity. It causes double-stranded DNA breakage and replication catastrophe, leading to apoptosis.
- Selective CHK1 inhibitor with Ki of 0.9 nM and IC50 of <1 nM
- Also inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM)
- Causes double-stranded DNA breakage
- Induces replication catastrophe and apoptosis
- Demonstrates potent anti-tumor activity
- Inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), and ARK5 (IC50=64 nM)
- Requires CDC25A and CDK2 to induce DNA damage
- Causes chromosomal fragmentation in HeLa cells
- Induces replication stress and depletes RPA2 available for DNA binding
- Shows tumor growth inhibition in xenografts
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