WT-161|cas 1206731-57-8

Cas No.:	1206731-57-8
Synonyms:	WT161; WT 161
SMILES:	O=C(N/N=C/C1=CC=C(N(C2=CC=CC=C2)C3=CC=CC=C3)C=C1)CCCCCCC(NO)=O
Formula:	C₂₇H₃₀N₄O₃
M.Wt:	458.55
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

WT161 selectively inhibits HDAC6 and dramatically increases levels of acetylated α-tubulin (Ac-α-tubulin) with little effect on global lysine acetylation. WT161 induces significant toxicity in all multiple myeloma cell lines tested, with IC50s between 1.5 and 4.7 µM . WT161 in combination with bortezomib triggers significant accumulation of polyubiquitinated proteins and cell stress, followed by caspase activation and apoptosis. More importantly, this combination treatment is effective in bortezomib-resistant cells and in the presence of bone marrow stromal cells, which have been shown to mediate multiple myeloma cell drug resistance.WT161 shows toxicity at 100 mg/kg i.p., but WT161 is well tolerated at 50 mg/kg i.p.. Bortezomib combined with WT161 demonstrates a significant antitumor effect.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47627	QTX125 TFA	QTX125 TFA is a potent and highly selective HDAC6 inhibitor. QTX125 TFA exhibits excellent selectivity over other HDACs. QTX125 has antitumor effects.
DC47626	HDAC/BET-IN-1	HDAC/BET-IN-1 displays submicromolar inhibitory activity against HDAC1 and 6 (IC50 = 0.163 μM and 0.067 μM), and BRD4 (Ki = 0.076 μM), and possess potent antileukemia activity.
DC47625	Dihydrochlamydocin	Dihydrochlamydocin is a Putative HDAC inhibitor.
DC47624	HDAC1/2-IN-3	HDAC1/2-IN-3 is a HDAC1 and HDAC2 inhibitor with IC50 values 0-5 and 5-10 nM, respectively.
DC47268	Ivaltinostat formic	Ivaltinostat (CG-200745) formic is a potent HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic induces apoptosis.
DC46045	KA2507 hydrochloride	KA2507 hydrochloride is a potent and highly selective inhibitor of HDAC6 (IC50=2.5 nM) with no significant toxicities. KA2507 hydrochloride shows antitumor efficacy and immune modulatory effects.
DC45388	Pomiferin	Pomiferin (NSC 5113) acts as an potential inhibitor of HDAC, with an IC50 of 1.05 μM, and also potently inhibits mTOR (IC50, 6.2 µM).
DC44140	FNDR-20123	FNDR-20123 is an orally active, safe and a first-in-class anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 inhibits HDAC1/2/3/6/8 (IC50=25/29/2/11/282 nM) and inhibits Class III HDAC isoforms at nanomolar concentrations.
DC44009	FNDR-20123 free base	FNDR-20123 free base is an orally active, safe and a first-in-class anti-malarial HDAC inhibitor with IC50s of 31 nM and 3 nM for Plasmodium and human HDAC, respectively. FNDR-20123 free base exerts anti-malarial activity against Plasmodium falciparum asexual stage (IC50=41 nM) and sexual blood stage (IC50=190 nM for male gametocytes). FNDR-20123 free base inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 (IC50=25, 29, 2, 11, and 282 nM, respectively) and inhibits Class III HDAC isoforms at nanomolar concentrations.
DC41974	Ac-Arg-Gly-Lys(Ac)-AMC	Ac-Arg-Gly-Lys(Ac)-AMC is a substrate for HDAC.