PF-3450074| CAS 1352879-65-2

Cas No.:	1352879-65-2
Chemical Name:	PF-3450074
Synonyms:	PF-74,PF 74,PF74,PF 3450074;PF-3450074
SMILES:	O=C(N[C@@H](CC1=CC=CC=C1)C(N(C)C2=CC=CC=C2)=O)CC3=C(C)NC4=C3C=CC=C4
Formula:	C₂₇H₂₇N₃O₂
M.Wt:	425.52
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle[1][2]. CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
Target:	HIV-1 (NL4.3 strain):0.72 μM (IC50)
In Vitro:	PF-3450074 (PF-74) exhibits anti-viral activities against HIV wild type NL4-3 and HIV T107N mutant with EC50 values of 0.72 μM and 4.5μM, respectively[1]. PF-3450074 (PF-74) displays a good potency in primary human peripheral blood mononuclear cells (PBMCs), inhibits HIV-193RW025, HIV-1JR-CSF and HIV-193MW965 with IC50 values of 1.5 ± 0.9 μM; 0.6 ± 0.20 μM; and 0.6 ± 0.10 μM, respectively. This compound shows Median IC50 and CC50 values of 0.9 ± 0.5 μM and 90.5 ± 5.9 μM, respectively[1]. The KD for the interaction between PF-74 and the CA hexamer, derived in the same manner as for NUP153, is determined to be 176 ± 78 nM[1]. PF-3450074 (PF-74) (10 μM; 8 hours) results in a marked reduction in late products of reverse transcription in HeLa-P4 cells with DNase I-treated stocks of Env-defective HIV-1 (R9.Env-)[2]. RT-PCR[2] Cell Line: HeLa-P4 cells Concentration: 10 μM Incubation Time: 8 hours Result: Inhibited HIV-1 reverse transcription in target cells.
References:	[1]. Xu JP, et al. Exploring Modifications of an HIV-1 Capsid Inhibitor: Design, Synthesis, and Mechanism of Action.J Drug Des Res. 2018;5(2). pii: 1070. Epub 2018 Aug 13. [2]. Shi J, et al. Small-molecule inhibition of human immunodeficiency virus type 1 infection by virus capsid destabilization.J Virol. 2011 Jan;85(1):542-9.

Cat. No.	Product name	Field of application
DC31074	Isopropyl myristate	Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC79609	NCGC00685960	NCGC00685960 is a Nicotinamide N-methyltransferase (NNMT) inhibitor with an IC50 < 10  nM. NCGC00685960 has potent antitumor activity. NCGC00685960 increases H3K27 trimethylation levels in ovarian cancer cells and inhibits α-SMA expression in NNMT-expressing ovarian fibroblasts. NCGC00685960 reduces 1-MNA levels, reverses SAM and H3K27 hypomethylation and significantly impairs collagen contractility in cancer-associated fibroblasts (CAFs). NCGC00685960 can be used for cancers research.
DC77831	Vicadrostat	Vicadrostat (compound 29 A) is a potent and selective inhibitor of aldosterone synthase(CYP11B2) with an IC50 of 16 nM. It exhibits potential in renal disease, diabetic nephropathy, cardiovascular diseases and fibrotic disorder research.
DC77813	Zeltociclib	Zeltociclib is a cyclin-dependent kinase inhibitor with antitumor effects.
DC77714	S3226	S3226 is an inhibitor for Na+/H+ exchange subtype 3 (NHE3) with an IC50 of 0.2 µmol/L in rat NHE3 transfected fibroblasts. S3226 exhibits protective activity in rat ischemia-induced acute renal failure models.
DC77387	AUR1545	AUR1545 is a selective degrader of KAT2A and KAT2B. AUR1545 can be used in the cancer research, including studies on AML (Acute myeloid leukemia), SCLC (Small-cell carcinoma), and NEPC (Neuroendocrine Prostate Cancer).
DC77822	JNJ-77242113 (Icotrokinr)	Icotrokinra (JNJ-77242113, JNJ-2113, PN-235) is an orally available and selective antagonist of the IL-23 receptor. It also inhibits IL-23–induced STAT3 phosphorylation in peripheral blood mononuclear cells with an IC50 of 5.6 pM and suppresses IL-23–induced IFN-γ production in NK cells with an IC50 of 18.4 pM. It also exhibits anti-inflammatory activity in a TNBS-induced colitis model in rats and holds potential for studying psoriasis, psoriatic arthritis, and inflammatory bowel disease.
DC77088	T025	T025 is as an orally available and potent inhibitor of Cdc2‐like kinases (CLKs) with an IC50s of 0.93 nM, 1 nM, 14 nM, 1.5 nM for CLK1, CLK2, CLK3, DYRK1B respectively. It exhibits anti‐tumor efficacy and can be used in MYC‐driven cancer research.
DC75868	AZ14133346	AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865	TI17	TI17 represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.