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MedKoo Cat#: 565383 | Name: BC-1382
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor which specifically disrupts the HECTD2/PIAS1 interaction.

Chemical Structure

BC-1382
BC-1382
CAS#1013753-99-5

Theoretical Analysis

MedKoo Cat#: 565383

Name: BC-1382

CAS#: 1013753-99-5

Chemical Formula: C23H29N3O5S

Exact Mass: 459.1828

Molecular Weight: 459.56

Elemental Analysis: C, 60.11; H, 6.36; N, 9.14; O, 17.41; S, 6.98

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,650.00 2 Weeks
1g USD 4,250.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
No Data
Synonym
BC1382; BC 1382; BC-1382
IUPAC/Chemical Name
(S)-N-(1-((2-Methoxybenzyl)amino)-1-oxopropan-2-yl)-1-(phenylsulfonyl)piperidine-4-carboxamide
InChi Key
RCWXKFCEGKXUIN-KRWDZBQOSA-N
InChi Code
InChI=1S/C23H29N3O5S/c1-17(22(27)24-16-19-8-6-7-11-21(19)31-2)25-23(28)18-12-14-26(15-13-18)32(29,30)20-9-4-3-5-10-20/h3-11,17-18H,12-16H2,1-2H3,(H,24,27)(H,25,28)/t17-/m0/s1
SMILES Code
O=C(C1CCN(S(=O)(C2=CC=CC=C2)=O)CC1)N[C@@H](C)C(NCC3=CC=CC=C3OC)=O
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
>3 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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
BC-1382 is an ubiquitin E3 ligase HECTD2 inhibitor.
In vitro activity:
BC-1382 was tested in an in vitro binding assay (Fig. 7C). The result suggested that BC-1382 is a potent inhibitor of HECTD2 with IC50 (median inhibitory concentration) ≈ 5 nM toward disrupting the HECTD2/PIAS1 interaction. BC-1382 drastically increased PIAS1 protein level in a nonstimulus condition with IC50 ≈100 nM (fig. S8B). PIAS3, PIAS4, and HECTD2 protein levels appeared to be unchanged. BC-1382 did not alter mRNA levels of PIAS1, PIAS4, or HECTD2 (fig. S8C). BC-1382 also improved PIAS1 protein stability by increasing its t1/2 (fig. S8D). BC-1382 suppressed LPS-induced PIAS1 degradation and restored PIAS1 protein levels at 800 nM (fig. S8E). Last, BC-1382 was able to suppress LPS-induced proinflammatory cytokines released by human peripheral blood mononuclear cells (PBMCs) (fig. S8F). Reference: Sci Transl Med. 2015 Jul 8;7(295):295ra109. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4706383/
In vivo activity:
To assess the in vivo anti-inflammatory activity of BC-1382, it was tested using P. aeruginosa– and LPS-induced pneumonia models. Briefly, C57BL/6J mice were challenged intratracheally with PA103 (104 CFU per mouse) or LPS (3 mg/kg). BC-1382 was given through intraperitoneal injection (10 mg/kg) at the same time. BC-1382 did not appear to affect BAL bacteria (Fig. 7D). However, it significantly decreased lavage protein concentrations, lavage cell counts, and cell infiltrates in both PA103-stimulated (Fig. 7, E, F, and H) and LPS-stimulated (fig. S9, A, B, and D) mice. Further, BC-1382 significantly decreased lavage cytokine levels in both models (Fig. 7G and fig. S9C). Reference: Sci Transl Med. 2015 Jul 8;7(295):295ra109. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4706383/

Preparing Stock Solutions

The following data is based on the product molecular weight 459.56 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. Coon TA, McKelvey AC, Lear T, Rajbhandari S, Dunn SR, Connelly W, Zhao JY, Han S, Liu Y, Weathington NM, McVerry BJ, Zhang Y, Chen BB. The proinflammatory role of HECTD2 in innate immunity and experimental lung injury. Sci Transl Med. 2015 Jul 8;7(295):295ra109. doi: 10.1126/scitranslmed.aab3881. PMID: 26157031; PMCID: PMC4706383.
In vitro protocol:
1. Coon TA, McKelvey AC, Lear T, Rajbhandari S, Dunn SR, Connelly W, Zhao JY, Han S, Liu Y, Weathington NM, McVerry BJ, Zhang Y, Chen BB. The proinflammatory role of HECTD2 in innate immunity and experimental lung injury. Sci Transl Med. 2015 Jul 8;7(295):295ra109. doi: 10.1126/scitranslmed.aab3881. PMID: 26157031; PMCID: PMC4706383.
In vivo protocol:
1. Coon TA, McKelvey AC, Lear T, Rajbhandari S, Dunn SR, Connelly W, Zhao JY, Han S, Liu Y, Weathington NM, McVerry BJ, Zhang Y, Chen BB. The proinflammatory role of HECTD2 in innate immunity and experimental lung injury. Sci Transl Med. 2015 Jul 8;7(295):295ra109. doi: 10.1126/scitranslmed.aab3881. PMID: 26157031; PMCID: PMC4706383.
1: Coon TA, McKelvey AC, Lear T, Rajbhandari S, Dunn SR, Connelly W, Zhao JY, Han S, Liu Y, Weathington NM, McVerry BJ, Zhang Y, Chen BB. The proinflammatory role of HECTD2 in innate immunity and experimental lung injury. Sci Transl Med. 2015 Jul 8;7(295):295ra109. doi: 10.1126/scitranslmed.aab3881. PubMed PMID: 26157031; PubMed Central PMCID: PMC4706383.