Organo-Metalloid Compounds
Medchemexpress LLC Abemaciclib (methanesulfonate) | 1231930-82-7 | 99.8% | 602.70 | 200 MG
This compound is a selective and BBB-permeable inhibitor of CDK4/6, with half-maximal inhibitory concentrations (IC50s) of 2 nM and 10 nM for CDK4 and CDK6, respectively.
- Selective inhibition of key enzymes involved in cell cycle regulation.
- Permeates the blood-brain barrier.
- Reduces cell viability in various human cell lines, including HCT-116, MCF7, and PANC-1.
- Inhibits Rb phosphorylation, leading to a G1 arrest and suppressed proliferation.
- Activity is specific for cells that are proficient in Rb.
- Effective in reducing cell viability across multiple cancer cell lines.
- Demonstrates antiproliferative activity against human HCT116 and MCF7 cells.
- Shows inhibition in resistant cell lines.
- Causes a cooperative antitumor effect when combined with other agents in xenograft models.
- Leads to significant tumor growth inhibition in xenograft models.
Medchemexpress LLC DPC-681 | 284661-68-3 | 99.7% | 669.85 | 10 MM * 1 ML
DPC-681 is a potent and selective inhibitor of HIV protease with IC90s for wild-type HIV-1 of 4 to 40 nM.
- Potent and selective inhibitor of HIV protease.
- Effective against wild-type HIV-1.
- Shows no loss in potency toward recombinant mutant HIVs with the D30N mutation.
- Exhibits a fivefold or smaller loss in potency toward mutant variants with three to five amino acid substitutions.
- Hepatic extraction can be saturated in dogs, leading to increased bioavailability at higher doses.
Medchemexpress LLC GGTI298 Trifluoroacetate | 1217457-86-7 | 99.9% | 593.66 | 5 MG
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor. It can inhibit Rap1A with an IC50 of 3 μM, while showing little effect on Ha-Ras with an IC50 of >20 μM. This compound appears as a white to yellow solid.
- Significantly reduces cAMP agonist-stimulated apical K+ conductance.
- Abolishes NF-κB activation, leading to sensitization of DR5-dependent apoptosis.
- Activates NF-κB and inhibits Akt.
- Reduces fluid accumulation in mouse ileal loop experiments.
- Store at 4°C, sealed, away from moisture.
- Soluble in DMSO at 100 mg/mL.
Medchemexpress LLC VH032-PEG5-C6-Cl (HaloPROTAC 2) | 1799506-06-1 | 99.9% | 783.41 | 100 MG
VH032-PEG5-C6-Cl (HaloPROTAC 2) is a conjugate that combines ligands for E3 ligase with a 21-atom-length linker. The linker's connector features a Halogen group, and the compound integrates a VH032-based VHL ligand with a 5-unit PEG linker. This product is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays. It is intended for research use only and is not sold to patients.
- Conjugate of ligands for E3 and a 21-atom-length linker.
- Connector of the linker is a Halogen group.
- Incorporates a VH032 based VHL ligand and a 5-unit PEG linker.
- Capable of inducing the degradation of GFP-HaloTag7 in cell-based assays.
- Treatment for 24 hours leads to nearly 70% degradation of GFP-Halotag7 at 2.5 μM.
Medchemexpress LLC AK-778-XXMU | 1227045-76-2 | 99.9% | C22H17ClN2O3 | 50 MG
AK-778-XXMU is a potent DNA binding inhibitor 2 (ID2) antagonist with a KD of 129 nM, used for the study of glioma. It inhibits the ID2-KDR signaling axis, leading to the downregulation of downstream angiogenic factors and invasion-related proteins, and the upregulation of the tumor suppressor factor PTEN. This compound demonstrates significant cancer-suppressing potency by inhibiting cell migration and invasion of glioma cell lines and inducing apoptosis.
- Potent ID2 antagonist with a KD of 129 nM
- Inhibits cell migration and invasion of glioma cell lines
- Induces apoptosis
- Inhibits ID2-KDR signaling axis
- Downregulates angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9)
- Upregulates tumor suppressor factor (PTEN)
Medchemexpress LLC AK-778-XXMU | 1227045-76-2 | 99.9% | C22H17ClN2O3 | 1 ML
AK-778-XXMU is a potent DNA binding inhibitor 2 (ID2) antagonist with a KD of 129 nM. It can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and exhibits significant cancer-suppressing potency. The compound acts by inhibiting the ID2-KDR signaling axis, leading to the down-regulation of angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9), and the up-regulation of the tumor suppressor factor (PTEN). It is suitable for the study of glioma.
- Potent ID2 antagonist with a KD of 129 nM
- Inhibits cell migration and invasion in glioma cell lines
- Induces apoptosis
- Exhibits significant cancer-suppressing potency
- Down-regulates angiogenic factors (VEGFA)
- Down-regulates invasion-related proteins (MMP2/9)
- Up-regulates tumor suppressor factor (PTEN)
- Inhibits tumor growth in U87 glioma xenograft mice model
Medchemexpress LLC AK-778-XXMU | 1227045-76-2 | 99.9% | C22H17ClN2O3 | 25 MG
AK-778-XXMU is a potent DNA binding inhibitor 2 (ID2) antagonist with a KD of 129 nM. It inhibits the ID2-KDR signaling axis, leading to the down-regulation of downstream angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9), while up-regulating the tumor suppressor factor (PTEN). It can inhibit cell migration and invasion of glioma cell lines, induce apoptosis, and demonstrates significant cancer-suppressing potency. This compound is used for the study of glioma.
- Potent DNA binding inhibitor 2 (ID2) antagonist
- Inhibits cell migration and invasion of glioma cell lines
- Induces apoptosis
- Demonstrates significant cancer-suppressing potency
- Inhibits ID2-KDR signaling axis
- Down-regulates angiogenic factors (VEGFA) and invasion-related proteins (MMP2/9)
- Up-regulates tumor suppressor factor (PTEN)
- Suitable for the study of glioma