HBX-41108
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MedKoo CAT#: 407460

CAS#: 924296-39-9

Description: HBX 41108 is an inhibitor of ubiquitin-specific protease (USP) 7. HBX 41108 inhibits USP7 deubiquitinating activity with an IC(50) in the submicromolar range. HBX 41,108 was shown to affect USP7-mediated p53 deubiquitination in vitro and in cells. As RNA interference-mediated USP7 silencing in cancer cells, HBX 41,108 treatment stabilized p53, activated the transcription of a p53 target gene without inducing genotoxic stress, and inhibited cancer cell growth. HBX 41,108 induced p53-dependent apoptosis as shown in p53 wild-type and null isogenic cancer cell lines.

Chemical Structure

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HBX-41108
CAS# 924296-39-9
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 407460
Name: HBX-41108
CAS#: 924296-39-9
Chemical Formula: C13H3ClN4O
Exact Mass: 266.00
Molecular Weight: 266.644
Elemental Analysis: C, 58.56; H, 1.13; Cl, 13.29; N, 21.01; O, 6.00

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1350 Ready to ship
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Synonym: HBX 41108; HBX-41108; HBX41108; HBX 41,108; HBX-41,108; HBX41,108.

IUPAC/Chemical Name: 7-Chloro-9-oxo-9H-indeno[1,2-b]pyrazine-2,3-dicarbonitrile

InChi Key: BIGPXXAUSQLTQR-UHFFFAOYSA-N

InChi Code: InChI=1S/C13H3ClN4O/c14-6-1-2-7-8(3-6)13(19)12-11(7)17-9(4-15)10(5-16)18-12/h1-3H

SMILES Code: N#CC1=C(C#N)N=C2C(C(C3=C2C=CC(Cl)=C3)=O)=N1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: HBX 41108 is an inhibitor of ubiquitin-specific protease (USP) 7 activity (IC50 = 424 nM). Also inhibits USP7-mediated p53 deubiquitination (IC50 = 0.8 μM).
In vitro activity: Moreover, the proportion of cells in the G0/G1 phase was significantly increased by AGEs, which was decreased by USP7 knockdown or HBX 41108, whereas that of cells in the S phase was significantly decreased by AGEs, which was increased by USP7 knockdown or HBX 41108 (Figure 2D,E). In addition, AGEs markedly increased the level of cell senescence, whereas the inhibition of USP7 by shUSP7 or HBX 41108 could reverse this effect (Figure 2F). p53 and p21 are markers of cell senescence. Western blot analysis revealed that the expressions of p53 and p21 were elevated by AGEs and decreased by shUSP7 and HBX 41108 (Figure 2G,H). These results indicated that inhibition of USP7 expression and its deubiquitinating activity could reduce cell cycle arrest and cell senescence in HUVECs. Reference: Acta Biochim Biophys Sin (Shanghai). 2022 Mar 25;54(3):311-320. https://pubmed.ncbi.nlm.nih.gov/35538032/
In vivo activity: Treatment of diabetic rats with HBX 41108 decreased blood glucose levels on 14 post-injury (Figure 5A). STZ (streptozotocin) significantly reduced the wound healing rate, whereas the application of HBX 41108 could rescue the STZ-mediated effects (Figure 5B,C). HE staining of tissue sections showed that epithelial tissue was newly formed in wounds treated with HBX 41108 on day 7 post-injury (Figure 5D). Meanwhile, on day 7 and day 14, the expressions of USP7, p53, and p21 were found to be increased by STZ and decreased by the application of HBX 41108 (Figure 5E). These results showed that HBX 41108 could facilitate wound healing in diabetic rats through inhibiting USP7 deubiquitinating activity. Reference: Acta Biochim Biophys Sin (Shanghai). 2022 Mar 25;54(3):311-320. https://pubmed.ncbi.nlm.nih.gov/35538032/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 25.0 93.76
DMSO 29.8 111.87
DMSO:PBS (pH 7.2) (1:40) 0.2 0.75

Preparing Stock Solutions

The following data is based on the product molecular weight 266.64 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Li X, Wang T, Tao Y, Wang X, Li L, Liu J. Inhibition of USP7 suppresses advanced glycation end-induced cell cycle arrest and senescence of human umbilical vein endothelial cells through ubiquitination of p53. Acta Biochim Biophys Sin (Shanghai). 2022 Mar 25;54(3):311-320. doi: 10.3724/abbs.2022003. PMID: 35538032.
In vitro protocol: 1. Li X, Wang T, Tao Y, Wang X, Li L, Liu J. Inhibition of USP7 suppresses advanced glycation end-induced cell cycle arrest and senescence of human umbilical vein endothelial cells through ubiquitination of p53. Acta Biochim Biophys Sin (Shanghai). 2022 Mar 25;54(3):311-320. doi: 10.3724/abbs.2022003. PMID: 35538032.
In vivo protocol: 1. Li X, Wang T, Tao Y, Wang X, Li L, Liu J. Inhibition of USP7 suppresses advanced glycation end-induced cell cycle arrest and senescence of human umbilical vein endothelial cells through ubiquitination of p53. Acta Biochim Biophys Sin (Shanghai). 2022 Mar 25;54(3):311-320. doi: 10.3724/abbs.2022003. PMID: 35538032.

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1: Nicholson B, Suresh Kumar KG. The multifaceted roles of USP7: new therapeutic
opportunities. Cell Biochem Biophys. 2011 Jun;60(1-2):61-8. doi:
10.1007/s12013-011-9185-5. Review. PubMed PMID: 21468693.


2: Colland F, Formstecher E, Jacq X, Reverdy C, Planquette C, Conrath S, Trouplin
V, Bianchi J, Aushev VN, Camonis J, Calabrese A, Borg-Capra C, Sippl W, Collura
V, Boissy G, Rain JC, Guedat P, Delansorne R, Daviet L. Small-molecule inhibitor
of USP7/HAUSP ubiquitin protease stabilizes and activates p53 in cells. Mol
Cancer Ther. 2009 Aug;8(8):2286-95. doi: 10.1158/1535-7163.MCT-09-0097. Epub 2009
Aug 11. PubMed PMID: 19671755.


3: Lee KW, Cho JG, Kim CM, Kang AY, Kim M, Ahn BY, Chung SS, Lim KH, Baek KH,
Sung JH, Park KS, Park SG. Herpesvirus-associated ubiquitin-specific protease
(HAUSP) modulates peroxisome proliferator-activated receptor γ (PPARγ) stability
through its deubiquitinating activity. J Biol Chem. 2013 Nov 15;288(46):32886-96.
doi: 10.1074/jbc.M113.496331. Epub 2013 Sep 26. PubMed PMID: 24072712; PubMed
Central PMCID: PMC3829140.