Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
24 Results for "
wild-type enzyme
" in MedChemExpress (MCE) Product Catalog:
Products (24)
24 Results for "wild-type enzyme" in MCE Product Catalog:
8
8 Publications Verification
Target:
Research Areas:
NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity .
3
Target:
Research Areas:
Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes .
1
Target:
Research Areas:
Trovirdine (LY300046) is a selective non-nucleoside HIV-1 reverse transcriptase inhibitor, with an IC50 value of 0.012 μM against the wild-type enzyme. Trovirdine inhibits the replication of both wild-type and mutant HIV-1, and exerts synergistic or additive effects when combined with some antiviral drugs. Trovirdine is applicable to research related to HIV-1 infection .
Target:
Research Areas:
ZLD1039 is a potent, highly selective, and orally bioavailable EZH2 inhibitor. ZLD1039 shows potent and concentration-dependent inhibition of PRC2 enzymatic activity against EZH2 wild-type as well as Y641F, and A677G mutant enzymes with IC50 values of 5.6, 15, and 4.0 nM, respectively. ZLD1039 inhibits breast tumor growth and metastasis .
Cat. No.: HY-131312
CAS No.: 2230263-60-0
Synonyms: LY3410738; Mutant IDH1-IN-6
Target:
Research Areas:
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes .
Cat. No.: HY-15350
CAS No.: 148311-89-1
Synonyms: LY 300046 hydrochloride
Target:
Research Areas:
Trovirdine hydrochloride (LY300046 hydrochloride) is a selective non-nucleoside HIV-1 reverse transcriptase inhibitor, with an IC50 value of 0.012 μM against the wild-type enzyme. Trovirdine hydrochloride inhibits the replication of both wild-type and mutant HIV-1, and exerts synergistic or additive effects when combined with some antiviral drugs. Trovirdine hydrochloride is applicable to research related to HIV-1 infection .
Cat. No.: HY-131312A
CAS No.: 2759438-85-0
Synonyms: LY3410738 gentisate; Mutant IDH1-IN-6 gentisate
Target:
Research Areas:
Crelosidenib (gentisate) is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50 of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Crelosidenib (gentisate) is less active at inhibiting the IDH wild-type enzymes .
Cat. No.: HY-19885
CAS No.: 955005-63-7
Research Areas:
AR-102 has inhibitory activity towards Staphylococcus aureus. AR-102 exhibits a competitive potent inhibition of the F98Y mutant DHFR (Ki = 0.22 nM). AR-102 has been determined as ternary complex with NADPH in both wild-type S. aureus DHFR and the TMP-resistant F98Y mutant enzyme .
Cat. No.: HY-16745A
CAS No.: 1433857-09-0
Synonyms: KRP-AM1977 hydrochloride
Lascufloxacin (KRP-AM1977) hydrochloride is a potent antibacterial compound candidate with broad-spectrum activity against various clinical isolates. Lascufloxacin hydrochloride shows the most potent activity against Gram-positive bacteria compared to other tested quinolones. Lascufloxacin hydrochloride demonstrates incomplete cross-resistance against existing quinolone-resistant strains. Lascufloxacin hydrochloride has potent inhibitory activity against both wild-type and mutated target enzymes.
Cat. No.: HY-167673
CAS No.: 1807639-36-6
Target:
Research Areas:
RNF5-IN-1 is a selective small-molecule inhibitor and degrader of the E3 ubiquitin ligase RNF5. RNF5-IN-1 directly binds to the N-terminal cytosolic domain of RNF5 with a KD of 594 nM, inhibits the E3 ubiquitin ligase activity of RNF5, and exhibits selectivity over Hrd1 and Praja1. RNF5-IN-1 promotes the degradation of RNF5 via the p97/VCP-dependent endoplasmic reticulum-associated degradation (ERAD) and proteasome pathway. RNF5-IN-1 inhibits the retrotranslocation of misfolded proteins. RNF5-IN-1 is applicable for research on mechanisms related to cystic fibrosis .
Cat. No.: HY-168069
Research Areas:
DHFR-IN-20 (Compound LA1) is a Plasmodium falciparum dihydrofolate reductase (DHFR) inhibitor, with Kis of 0.16, 0.30, 6.6 nM for PfDHFR-WT, PfDHFR-QM, HsDHFR. DHFR-IN-20 has antimalarial activities (IC50: 1.4 nM and 1.6 μM for P. falciparum carrying the wild-type (TM4/8.2) and the quadruple mutant (V1/S) PfDHFR enzyme .
Cat. No.: HY-176210
Target:
Research Areas:
CYP51-IN-24 (Compound 22) is a Sterol 14α-Demethylase (CYP51) inhibitor. CYP51-IN-24 exhibits potent inhibitory activity against wild-type and drug-resistant fungi. CYP51-IN-24 inhibits ergosterol biosynthesis by binding to the fungal CYP51 enzyme. CYP51-IN-24 can be used in research and drug development against drug-resistant fungal infections .
Cat. No.: HY-162720
Research Areas:
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg) .
Cat. No.: HY-181263
Target:
Research Areas:
Jun13698 is a SARS-CoV-2 main protease (M pro) inhibitor with Ki values of 65.6 nM, 510.0 nM, and 117.5 nM against the wild-type, E166V, and E166A mutants, respectively. Jun13698 forms stable complexes with wild-type and mutant M pro to mediate enzyme inhibition. Jun13698 exhibits antiviral activity against SARS-CoV-2 variants carrying the E166V/A mutation. Jun13698 is applicable to COVID-19-related research .
Cat. No.: HY-182792
CAS No.: 2412966-86-8
Synonyms: TERN-701
Embibatinib (TERN-701) is an orally active and allosteric BCR-ABL1 tyrosine kinase inhibitor targeting the myristoyl pocket. Embibatinib exhibits an IC50 of 0.38 nM against ABL1 wild-type enzyme. Embibatinib can be used for the study of chronic myeloid leukemia (CML) .
Cat. No.: HY-123153
CAS No.: 1816331-64-2
Target:
Research Areas:
GSK990 is an inactive mutant IDH1 inhibitor with no significant inhibitory activity against wild-type or mutant IDH1/IDH2 enzymes. In experiments, GSK990 can serve as an inactive negative control for the IDH1 inhibitor GSK321 (HY-18948). GSK990 is applicable to the research of acute myeloid leukemia .
Cat. No.: HY-123883
CAS No.: 865298-81-3
Target:
Research Areas:
MK-0536 is a highly potent HIV-1 integrase inhibitor that effectively suppresses the replication of wild-type viruses. MK-0536 retains significant antiviral activity against multiple key drug-resistant mutants such as Y143R and N155H, and shows no toxicity to uninfected cells. MK-0536 selectively blocks the strand transfer reaction of integrase by chelating magnesium ions at the active site and interacting with viral DNA and enzyme residues. MK-0536 is applicable to the study of HIV infection mechanisms .
Cat. No.: HY-184735
CAS No.: 2924270-62-0
Target:
Research Areas:
Antifungal agent-170 is an Antifungal agent. Antifungal agent-170 potently inhibits the growth of recombinant Saccharomyces cerevisiae strains expressing wild-type and mutant fungal CYP51 enzymes. Antifungal agent-170 potently inhibits the growth of Candida albicans, Candida glabrata, Candida krusei, Cryptococcus neoformans and Cryptococcus gattii. Antifungal agent-170 provides survival benefits in the Galleria mellonella (greater wax moth) infection model. Antifungal agent-170 can be used for the research of invasive fungal infections .
- 1
- 2
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
